Chemicals and Drugs
Azetidines
Azetidines

Lipoprotein-associated phospholipase A2, platelet-activating factor acetylhydrolase, generates two bioactive products during the oxidation of low-density lipoprotein: use of a novel inhibitor. (1/572)

A novel and potent azetidinone inhibitor of the lipoprotein-associated phospholipase A2 (Lp-PLA2), i.e. platelet-activating factor acetylhydrolase, is described for the first time. This inhibitor, SB-222657 (Ki=40+/-3 nM, kobs/[I]=6. 6x10(5) M-1.s-1), is inactive against paraoxonase, is a poor inhibitor of lecithin:cholesterol acyltransferase and has been used to investigate the role of Lp-PLA2 in the oxidative modification of lipoproteins. Although pretreatment with SB-222657 did not affect the kinetics of low-density lipoprotein (LDL) oxidation by Cu2+ or an azo free-radical generator as determined by assay of lipid hydroperoxides (LOOHs), conjugated dienes and thiobarbituric acid-reacting substances, in both cases it inhibited the elevation in lysophosphatidylcholine content. Moreover, the significantly increased monocyte chemoattractant activity found in a non-esterified fatty acid fraction from LDL oxidized by Cu2+ was also prevented by pretreatment with SB-222657, with an IC50 value of 5.0+/-0.4 nM. The less potent diastereoisomer of SB-222657, SB-223777 (Ki=6.3+/-0.5 microM, kobs/[I]=1.6x10(4) M-1.s-1), was found to be significantly less active in both assays. Thus, in addition to generating lysophosphatidylcholine, a known biologically active lipid, these results demonstrate that Lp-PLA2 is capable of generating oxidized non-esterified fatty acid moieties that are also bioactive. These findings are consistent with our proposal that Lp-PLA2 has a predominantly pro-inflammatory role in atherogenesis. Finally, similar studies have demonstrated that a different situation exists during the oxidation of high-density lipoprotein, with enzyme(s) other than Lp-PLA2 apparently being responsible for generating lysophosphatidylcholine.  (+info)

Characterization and expression of the mouse Hsc70 gene. (2/572)

A genomic clone encoding the mouse Hsc70 gene has been isolated and characterized by DNA sequence analysis. The gene is approximately 3. 9 kb in length and contains eight introns, the fifth, sixth and eighth of which encode the three U14 snoRNAs. The gene has been located on Chr 9 in the order Fli1-Itm1-Olfr7-Hsc70(Rnu14)-Cbl by genetic analysis. Expression of Hsc70 is universal in all tissues of the mouse, but is slightly elevated in liver, skeletal muscle and kidney tissue, while being depressed in testes. In cultured mouse NIH 3T3 cells or human HeLa cells, Hsc70 mRNA levels are low under normal conditions, but can be induced 8-fold higher in both lines by treatment with the amino acid analog azetidine. A similar induction is seen in cells treated with the proteosome inhibitor MG132 suggesting that elevated Hsc70 expression may be coupled to protein degradation. Surprisingly, expression of the human Hsc70 gene is also regulated by cell-cycle position being 8-10-fold higher in late G1/S-phase cells as opposed to the levels in early G1-phase cells.  (+info)

Intron-independent association of splicing factors with active genes. (3/572)

The cell nucleus is organized as discrete domains, often associated with specific events involved in chromosome organization, replication, and gene expression. We have examined the spatial and functional relationship between the sites of heat shock gene transcription and the speckles enriched in splicing factors in primary human fibroblasts by combining immunofluorescence and fluorescence in situ hybridization (FISH). The hsp90alpha and hsp70 genes are inducibly regulated by exposure to stress from a low basal level to a high rate of transcription; additionally the hsp90alpha gene contains 10 introns whereas the hsp70 gene is intronless. At 37 degrees C, only 30% of hsp90alpha transcription sites are associated with speckles whereas little association is detected with the hsp70 gene, whose constitutive expression is undetectable relative to the hsp90alpha gene. Upon exposure of cells to heat shock, the heavy metal cadmium, or the amino acid analogue azetidine, transcription at the hsp90alpha and hsp70 gene loci is strongly induced, and both hsp transcription sites become associated with speckles in >90% of the cells. These results reveal a clear disconnection between the presence of intervening sequences at specific gene loci and the association with splicing factor-rich regions and suggest that subnuclear structures containing splicing factors are associated with sites of transcription.  (+info)

Influence of 1-[(E)-2-(2-methyl-4-nitrophenyl)diaz-1-enyl]pyrrolidine-2-carboxylic acid and diphenyliodonium chloride on ruminal protein metabolism and ruminal microorganisms. (4/572)

The effects of 1-[(E)-2-(2-methyl-4-nitrophenyl)diaz-1-enyl]pyrrolidine-2-carboxy lic acid (LY29) and diphenyliodonium chloride (DIC) on the degradation of protein to ammonia were determined in a mixed rumen microbial population taken from sheep on a grass hay-concentrate diet. Both compounds decreased NH3 production by inhibiting deamination of amino acids. LY29, but not DIC, inhibited growth of the high-activity ammonia-producing species, Clostridium aminophilum and Clostridium sticklandii.  (+info)

Imaging central nicotinic acetylcholine receptors in baboons with [18F]fluoro-A-85380. (5/572)

Central nicotinic acetylcholine receptors (nAChRs) have been implicated in learning-memory processes. Postmortem brain tissue of patients who suffered senile dementia or Parkinson's disease shows low density of nAChRs. In this study, we used PET to evaluate the distribution and kinetics of the fluoro derivative of the high-affinity and alpha4beta2-subtype-selective, nicotinic ligand 3-[2(S)-2-azetidinylmethoxy]pyridine (A-85380) in baboons. METHODS: After intravenous injection of 37 MBq (1 mCi, 1-1.5 nmol) [18F]fluoro-A-85380 into isoflurane-anesthetized baboons, dynamic PET data were acquired for 180 min. Time-activity curves were generated from regions of interest. Displacement experiments (80 min after injection of the radiotracer) were performed using cytisine (1 mg/kg subcutaneously) and unlabeled fluoro-A-85380 (0.1 and 0.3 mg/kg intravenously). Toxicological studies were performed in mice. RESULTS: Brain radioactivity reached a plateau within 40-50 min of injection of the tracer. In the thalamic area, radioactivity remained constant for 180 min, while clearance from the cerebellum was slow (t1/2 = 145-190 min). Cytisine and unlabeled fluoro-A-85380 reduced brain radioactivity at 180 min by 50%-60%, 30%-35% and 20%-35% of control values in the thalamus, cerebellum and frontal cortex, respectively. A slight, transient increase (20 mm Hg) in blood pressure was observed with the highest displacing dose of unlabeled fluoro-A-85380. Lethal dose in mice was found to be 2.2 mg/kg intravenously. CONCLUSION: These results demonstrate the feasibility and the safety of imaging nAChRs in vivo using labeled or unlabeled fluoro-A-85380.  (+info)

Novel TRH analog improves motor and cognitive recovery after traumatic brain injury in rodents. (6/572)

Thyrotropin-releasing hormone (TRH) and certain TRH analogs show substantial neuroprotective effects in experimental brain or spinal cord trauma but also have other physiological actions (autonomic, analeptic, and endocrine) that may be undesirable for the treatment of neurotrauma in humans. We developed a novel TRH analog (2-ARA-53a), with substitutions at the NH(2)-terminus and imidazole ring, that preserves the neuroprotective action of TRH-like compounds while decreasing or eliminating their autonomic, analeptic, and endocrine effects. Rats administered 2-ARA-53a (1.0 mg/kg, n = 17) intravenously 30 min after lateral fluid percussion brain injury showed marked improvement in motor recovery compared with vehicle-treated controls (n = 14). Treatment of mice subjected to moderate controlled cortical impact brain injury, at the same dose and time after trauma (n = 8), improved both motor recovery and cognitive performance in a water maze place learning task compared with vehicle-treated controls (n = 8). In injured rats, no autonomic or analeptic effects were observed with this compound, and endocrine effects were significantly reduced with 2-ARA-53a, in contrast to those found with a typical NH(2)-terminal-substituted TRH analog (YM-14673). These findings demonstrate that the neuroprotective effects of TRH-related compounds can be dissociated from their other major physiological actions and suggest a potential role for dual-substituted TRH analogs in the treatment of clinical neurotrauma.  (+info)

Lipoprotein-associated phospholipase A(2), platelet-activating factor acetylhydrolase, is expressed by macrophages in human and rabbit atherosclerotic lesions. (7/572)

We studied the expression of lipoprotein-associated phospholipase A(2) (Lp-PLA(2)), an enzyme capable of hydrolyzing platelet-activating factor (PAF), PAF-like phospholipids, and polar-modified phosphatidylcholines, in human and rabbit atherosclerotic lesions. Oxidative modification of low-density lipoprotein, which plays an important role in atherogenesis, generates biologically active PAF-like modified phospholipid derivatives with polar fatty acid chains. PAF is known to have a potent proinflammatory activity and is inactivated by its hydrolysis. On the other hand, lysophosphatidylcholine and oxidized fatty acids released from oxidized low-density lipoprotein as a result of Lp-PLA(2) activity are thought to be involved in the progression of atherosclerosis. Using combined in situ hybridization and immunocytochemistry, we detected Lp-PLA(2) mRNA and protein in macrophages in both human and rabbit atherosclerotic lesions. Reverse transcriptase-polymerase chain reaction analysis indicated an increased expression of Lp-PLA(2) mRNA in human atherosclerotic lesions. In addition, approximately 6-fold higher Lp-PLA(2) activity was detected in atherosclerotic aortas of Watanabe heritable hyperlipidemic rabbits compared with normal aortas from control rabbits. It is concluded that (1) macrophages in both human and rabbit atherosclerotic lesions express Lp-PLA(2), which could cleave any oxidatively modified phosphatidylcholine present in the lesion area, and (2) modulation of Lp-PLA(2) activity could lead to antiatherogenic effects in the vessel wall.  (+info)

Activation of spinal wide dynamic range neurons by intracutaneous microinjection of nicotine. (8/572)

Nicotine evokes pain in the skin and oral mucosa and excites a subpopulation of cutaneous nociceptors, but little is known about the central transmission of chemogenic pain. We have investigated the responses of lumbar spinal wide dynamic range (WDR)-type dorsal horn neurons to intracutaneous (ic) microinjection of nicotine in pentobarbital-anesthetized rats. Nearly all (97%) units responded to nicotine microinjected ic (1 microl) into the low-threshold region of the hind-paw mechanosensitive receptive field in a concentration-related manner (0.01-10%). Responses to repeated injections of 10% nicotine exhibited tachyphylaxis at 5-, 10-, and 15-min interstimulus intervals. Significant tachyphylaxis was not seen with 1% nicotine. All nicotine-responsive units tested (n = 30) also responded to ic histamine (1 microl, 3%) and did not exhibit tachyphylaxis to repeated histamine. However, there was significant cross-tachyphylaxis of nicotine to histamine. Thus 5 min after ic nicotine, histamine-evoked responses were attenuated significantly compared with the initial histamine-evoked response prior to nicotine, with partial recovery over the ensuing 15 min. Neuronal excitation by ic nicotine was not mediated by histamine H1 receptors because ic injection of the H1 receptor antagonist, cetirizine, had no effect on ic nicotine-evoked responses, whereas it significantly attenuated ic histamine-evoked responses in the same neurons. The lowest-threshold portion of cutaneous receptive fields showed a significant expansion in area at 20 min after ic nicotine 10%, indicative of sensitization. Responses to 1% nicotine were significantly reduced after ic injection of the nicotinic antagonist, mecamylamine (0.1% ic), with no recovery over the ensuing 40-60 min. These data indicate that nicotine ic excites spinal WDR neurons, partly via neuronal nicotinic acetylcholine receptors that are presumably expressed in cutaneous nociceptor terminals. Repeated injections of high concentrations of nicotine led to tachyphylaxis and cross-tachyphylaxis with histamine, possibly relevant to peripheral analgesic effects of nicotine.  (+info)

Cost-effectiveness of Simvastatin plus Ezetimibe for Cardiovascular Prevention in CKD: Results of the Study of Heart and Renal...
© 2015 The Authors. Background: Simvastatin, 20. mg, plus ezetimibe, 10. mg, daily (simvastatin plus ezetimibe) reduced major atherosclerotic events in patients with moderate to severe chronic kidney disease (CKD) in the Study of Heart and Renal Protection (SHARP), but its cost-effectiveness is unknown. Study Design: Cost-effectiveness of simvastatin plus ezetimibe in SHARP, a randomized controlled trial. Setting & Population: 9,270 patients with CKD randomly assigned to simvastatin plus ezetimibe versus placebo; participants in categories by 5-year cardiovascular risk (low,|10%; medium, 10%-|20%; or high,≥20%) and CKD stage (3, 4, 5 not on dialysis, or on dialysis therapy). Model, Perspective, & Timeline: Assessment during SHARP follow-up from the UK perspective; long-term projections. Intervention: Simvastatin plus ezetimibe (2015 UK £1.19 per day) during 4.9 years median follow-up in SHARP; scenario analyses with high-intensity statin regimens (2015 UK £0.05-£1.06 per day). Outcomes:
https://www.mrc-phru.ox.ac.uk/publications/575273
Synthesis and Bioactivities of 2-Azetidinone Derivatives as Cholesterol Absorption Inhibitors | Bentham ScienceSynthesis and Bioactivities of 2-Azetidinone Derivatives as Cholesterol Absorption Inhibitors | Bentham Science
Title: Synthesis and Bioactivities of 2-Azetidinone Derivatives as Cholesterol Absorption Inhibitors. VOLUME: 7 ISSUE: 6. Author(s):Yubin Wang, Hai Qian, Jinpei Zhou, Huibin Zhang, Jianfeng Ji and Wenlong Huang. Affiliation:Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.. Keywords:2-Azetidinones, cholesterol absorption inhibitor, synthesis, bioactivities, hamsters, cardiovascular research, coronary heart disease (CHD), exogenous pathways, 3-methylglutaryl, 3-hydroxy. Abstract: Twenty-four 2-azetidinone derivatives have been designed and synthesized as cholesterol absorption inhibitors. All new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed considerable effects in lowering the levels of total cholesterol in the serum, especially compound 2d, 4a, 4f, 4i and 4j. ...
https://www.eurekaselect.com/89023/article/synthesis-and-bioactivities-2-azetidinone-derivatives-cholesterol-absorption?tracking-code=4
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Ezetimibe is a potent cholesterol absorption inhibitor that lowers LDL cholesterol and raises HDL cholesterol in hypercholesterolemic humans (4) and is now in phase III clinical trials. Preclinical studies have demonstrated that ezetimibe selectively inhibits the transport of radiolabeled cholesterol through the intestinal wall and ultimately into the plasma (1,3). The precise molecular mechanism by which cholesterol is absorbed in the intestine (and how ezetimibe inhibits this absorption) is currently unknown and under intensive investigation.. In the present studies, we demonstrated that feeding high-fat diets containing modest cholesterol to hamsters leads to obesity accompanied by hyperinsulinemia, hyperleptinemia, hypercholesterolemia, and hypertriglyceridemia, which are characteristic of the profile often observed in obese insulin-resistant and/or type 2 diabetic patients (9). In an initial report, we described the potent cholesterol absorption inhibitor ezetimibe, which inhibited the rise ...
http://diabetes.diabetesjournals.org/content/50/6/1330
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The effects of lowering LDL cholesterol with simvastatin plus ezetimibe in patients with chronic kidney disease (Study of Heart...
BACKGROUND: Lowering LDL cholesterol with statin regimens reduces the risk of myocardial infarction, ischaemic stroke, and the need for coronary revascularisation in people without kidney disease, but its effects in people with moderate-to-severe kidney disease are uncertain. The SHARP trial aimed to assess the efficacy and safety of the combination of simvastatin plus ezetimibe in such patients. METHODS: This randomised double-blind trial included 9270 patients with chronic kidney disease (3023 on dialysis and 6247 not) with no known history of myocardial infarction or coronary revascularisation. Patients were randomly assigned to simvastatin 20 mg plus ezetimibe 10 mg daily versus matching placebo. The key prespecified outcome was first major atherosclerotic event (non-fatal myocardial infarction or coronary death, non-haemorrhagic stroke, or any arterial revascularisation procedure). All analyses were by intention to treat. This trial is registered at ClinicalTrials.gov, NCT00125593, and
https://www.ndph.ox.ac.uk/publications/166703
Cholesterol absorption inhibitor - WikipediaCholesterol absorption inhibitor - Wikipedia
Cholesterol absorption inhibitors are a class of compounds that prevents the uptake of cholesterol from the small intestine into the circulatory system. Most of these molecules are monobactams but show no antibiotic activity. An example is ezetimibe (SCH 58235) Another example is Sch-48461. The Sch is for Schering-Plough, where these compounds were developed. Phytosterols are also cholesterol absorption inhibitors. There are two sources of cholesterol in the upper intestine: dietary (from food) and biliary (from bile). Dietary cholesterol, in the form of lipid emulsions, combines with bile salts, to form bile salt micelles from which cholesterol can then be absorbed by the intestinal enterocyte. Once absorbed by the enterocyte, cholesterol is reassembled into intestinal lipoproteins called chylomicrons. These chylomicrons are then secreted into the lymphatics and circulated to the liver. These cholesterol particles are then secreted by the liver into the blood as VLDL particles, precursors to ...
https://en.wikipedia.org/wiki/Cholesterol_absorption_inhibitor
Abstract 330: Ezetimibe Prevents Atherogenesis Through Increased Catabolism and Fecal Excretion of LDL-cholesterol and Reduced...Abstract 330: Ezetimibe Prevents Atherogenesis Through Increased Catabolism and Fecal Excretion of LDL-cholesterol and Reduced...
Background: Intestinal cholesterol absorption inhibitor ezetimibe (EZE) added to a statin therapy has demonstrated benefits in the IMPROVE-IT trial by further reducing LDL-cholesterol levels than statin therapy alone. We investigated the mechanisms by which EZE could contribute to cardiovascular events reduction in apolipoprotein E knock-out (apoE ko) mice.. Methods: ApoE ko mice were fed a Paigen diet without (control) or with EZE (7mg/kg/day) for 6 weeks. To evaluate the effects of EZE on LDL-cholesterol metabolism and excretion, a first set of mice was injected intravenously with 3H-cholesteryl oleate labeled human LDL. A second set of mice was used for in vivo SPECT/CT imaging of 99mTc-cAbVCAM1-5, a single domain antibody directed against the Vascular Cell Adhesion Molecule-1 (VCAM-1), which was used as a marker of inflamed atherosclerotic plaques. The same mice were sacrificed for autoradiography and histology of aortic atherosclerotic plaques.. Results: Compared with control, EZE treatment ...
http://atvb.ahajournals.org/content/35/Suppl_1/A330
Abstract 14142: NPC1L1 Inhibition with Ezetimibe Suppresses Enhanced Formation of Aortic Atherosclerosis Induced by Dietary...Abstract 14142: NPC1L1 Inhibition with Ezetimibe Suppresses Enhanced Formation of Aortic Atherosclerosis Induced by Dietary...
Background: Dietary cholesterol oxidation products (oxysterols) are known to be absorbed and incorporate into lipoprotein in blood and atherosclerotic lesions and to accelerate the formation of atherosclerosis in animals. However, the mechanism of enhanced atherogenesis induced by dietary oxysterols has not been explored.. Aim: The aims of this study are to investigate molecular and cellular mechanisms of atherogenesis induced by dietary oxysterols and to examine therapeutic effects of a cholesterol absorption inhibitor ezetimibe.. Methods and Results: ApoE-deficient mice were fed either a control high-fat diet (control-HFD) or HFD containing oxysterols (oxysterol-HFD; 6.8 % of cholesterol was oxidized) for 8 weeks and infused with angiotensin II. Compared to control-HFD, dietary oxysterol-HFD enhanced the formation of aortic atherosclerosis, macrophage infiltration, lipid accumulation, immunoreactive MCP-1, and activated MMPs in atherosclerotic lesions without affecting plasma lipid levels ...
http://circ.ahajournals.org/content/122/Suppl_21/A14142
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Leicester Research Archive: A randomised placebo-controlled double-blind trial to evaluate lipid-lowering pharmacotherapy on...
Modulation of abdominal aortic aneurysm (AAA) expansion by HMG-CoA reductase inhibitors (statins) might be linked to reducing IL-6 and MMP-9, which may be consequent on reducing plasma cholesterol. Ezetimibe is a novel cholesterol absorption inhibitor used in combination with statins. This pilot study compared the biological effects of ezetimibe combination therapy with simvastatin alone on parameters relevant to aneurysm expansion including cytokines and proteolytic enzymes ...
https://lra.le.ac.uk/handle/2381/23506
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Ezetimibe: New perspectives in lipid lowering treatment | Jankowski | Cardiology JournalEzetimibe: New perspectives in lipid lowering treatment | Jankowski | Cardiology Journal
Therapeutic goals for lipid lowering treatment in the prevention of ischemic heart disease are often not reached in clinical practice. Even the highest doses of statins do not guarantee good control of hypercholesterolemia in all patients. Therefore, new lipid lowering drugs are being investigated. One of them is ezetimibe - intestinal cholesterol absorption inhibitor. Treatment with ezetimibe results in significant reduction of total cholesterol and LDL cholesterol levels. It is hoped that concomitant treatment with ezetimibe and other lipid lowering drugs (particularly statins) will be more effective. In large randomized clinical trials, co-administration of ezetimibe with atorvastatin and simvastatin proved to be more effective in lowering cholesterol levels and reaching target therapeutic levels than treatment with statin alone. In addition, combined treatment with ezetimibe and simvastatin was more effective compared to treatment with todays most effectively used statin (rosuvastatin) ...
https://journals.viamedica.pl/cardiology_journal/article/view/21699
PRIME PubMed | Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with...PRIME PubMed | Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with...
PubMed journal article Long-term safety and, tolerability profiles and lipid-modifying efficacy of ezetimibe coadministered with ongoing simvastatin treatment: a multicenter, randomized, double-blind, placebo-controlled, 48-week extension stud were found in PRIME PubMed. Download Prime PubMed App to iPhone or iPad.
https://www.unboundmedicine.com/medline/citation/15811480/Long_term_safety_and_tolerability_profiles_and_lipid_modifying_efficacy_of_ezetimibe_coadministered_with_ongoing_simvastatin_treatment:_a_multicenter_randomized_double_blind_placebo_controlled_48_week_extension_study_
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Comparison of Co-administration of Ezetimibe Plus Simvastatin Versus Simvastatin Alone in Primary Hypercholesterolemia (P03476)...Comparison of Co-administration of Ezetimibe Plus Simvastatin Versus Simvastatin Alone in Primary Hypercholesterolemia (P03476)...
Subjects must have documented coronary heart disease (CHD). For the purposes of this study, CHD will include one or more of the following features: documented stable angina (with evidence of ischemia on exercise testing); history of myocardial infarction; history of percutaneous coronary intervention (primarily PTCA with or without stent placement); symptomatic peripheral vascular disease (claudication); documented history of atherothrombotic cerebrovascular disease; and/or documented history of unstable angina or non-Q wave myocardial infarction ...
https://clinicaltrials.gov/show/NCT00651274
Comparison of Co-administration of Ezetimibe Plus Simvastatin Versus Simvastatin Alone in Primary Hypercholesterolemia (P03476)...Comparison of Co-administration of Ezetimibe Plus Simvastatin Versus Simvastatin Alone in Primary Hypercholesterolemia (P03476)...
Subjects must have documented coronary heart disease (CHD). For the purposes of this study, CHD will include one or more of the following features: documented stable angina (with evidence of ischemia on exercise testing); history of myocardial infarction; history of percutaneous coronary intervention (primarily PTCA with or without stent placement); symptomatic peripheral vascular disease (claudication); documented history of atherothrombotic cerebrovascular disease; and/or documented history of unstable angina or non-Q wave myocardial infarction ...
https://clinicaltrials.gov/ct2/show/NCT00651274
Analyses of cancer data from three ezetimibe trials. - MRCPHRU
BACKGROUND: Five years of statin therapy lowers low-density lipoprotein (LDL) cholesterol substantially and, over a 5-year period, results in reductions in the incidence of cardiovascular events. The Simvastatin and Ezetimibe in Aortic Stenosis (SEAS) trial (ClinicalTrials.gov number, NCT00092677) has raised the hypothesis that adding ezetimibe to statin therapy for larger LDL cholesterol reductions might increase the incidence of cancer. METHODS: We compared the results of a hypothesis-generating analysis of the incidence of cancer in the SEAS trial of ezetimibe plus simvastatin in 1873 patients (mean follow-up after ezetimibe or matching placebo was begun, 4.1 years) with a hypothesis-testing analysis of cancer data from the two large ongoing trials of this regimen: the Study of Heart and Renal Protection (SHARP) (NCT00125593) with 9264 patients (mean follow-up, 2.7 years) and the Improved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) (NCT00202878), currently with 11,353
https://www.mrc-phru.ox.ac.uk/publications/34368
Renal Fellow Network: Comparative Benefit of Ezetimibe plus Simvastatin in Individuals with Moderately Reduced eGFRRenal Fellow Network: Comparative Benefit of Ezetimibe plus Simvastatin in Individuals with Moderately Reduced eGFR
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http://renalfellow.blogspot.com/2017/05/comparative-benefit-of-ezetimibe-plus.html
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Ezetimibe Inhibits Hepatic Niemann-Pick C1-Like 1 to Facilitate Macrophage Reverse Cholesterol Transport in MiceSignificance |...Ezetimibe Inhibits Hepatic Niemann-Pick C1-Like 1 to Facilitate Macrophage Reverse Cholesterol Transport in MiceSignificance |...
In this study, we have shown that after peritoneal injection of [3H]-cholesterol-labeled mouse primary peritoneal macrophages, L1-KO mice expressing hepatic NPC1L1 (L1LivOnly) accumulated more [3H]-tracer in blood and tissues and secreted significantly reduced amounts of [3H]-neutral sterols in gallbladder bile and feces, when compared with L1-KO mice expressing no hepatic NPC1L1. Ezetimibe treatment reversed the accumulation of [3H]-tracer in blood and tissues and restored biliary and fecal excretion of [3H]-neutral sterols in L1LivOnly mice. Our results demonstrate an essential role of biliary sterol secretion in mediating macrophage-to-feces RCT in mice deficient in intestinal cholesterol absorption. Given that human livers express NPC1L1,8,10,15 our findings suggest that ezetimibe may have a previously unappreciated action: promoting macrophage RCT via direct inhibition of hepatic NPC1L1 in humans.. Recent studies on mice genetically or surgically deficient in biliary cholesterol secretion ...
http://atvb.ahajournals.org/content/33/5/920
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This trial will compare the efficacy and tolerability of atorvastatin, alone or in combination with ezetimibe, in patients with hypercholesterolaemia.
http://adisinsight.springer.com/trials/700052594?error=cookies_not_supported&code=d1ee6174-bc75-4b51-bce6-667557b94ec8
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The heterocycle moieties form the site of reaction in many enzymes and co-enzymes and also act as an important pharmacophore in the pharmaceutical drug designs. 2-Azetidinones are the 2-carbonyl derivatives of azetidine, more commonly known as ?-lactams. These structural entities occupied a central role in the vigil against bacterial infections over the past few decades. A subclass of these heterocyclic systems, monobactams or monocyclic ?-lactam derivatives exhibits several biological activities including antibacterial, antifungal, antiprotozoal, anti-mycobacterial, anti-HIV, antiviral, antimalarial, antioxidant, apoptotic inhibitors, anti-inflammatory activity, anticancer activity, herbicidal activity, etc. Monobactams has resistant to the ?-lactamase enzyme and could be a reasonable starting point for developing new drugs or inhibitors. In the present review, pharmacological activities of monocyclic ?-lactam derivatives have been discussed with respect to current research in the ...
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The article reports on a warning issued by the U.S. Food and Drug Administration (FDA) about the possible relationship between combination simvastatin plus ezetimibe and an increased incidence of cancer. According to preliminary data from the Simvastatin Ezetimibe Aortic Stenosis (SEAS) trial, the combination of simvastatin and ezetimibe lowered the low-density lipoprotein (LDL) levels of patients with mild to moderate aortic stenosis ...
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Azetidine Hydrochloride (CAS 36520-39-5) Market Research Report 2017Azetidine Hydrochloride (CAS 36520-39-5) Market Research Report 2017
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Efficacy of ezetimibe on improvement of glucose metabolism in Japanese subjects with type 2 diabetes. - AdisInsightEfficacy of ezetimibe on improvement of glucose metabolism in Japanese subjects with type 2 diabetes. - AdisInsight
This trial will investigate the effect of ezetimibe on glucose metabolism in patients with type 2 diabetes mellitus and hypercholesterolaemia. The primary
http://adisinsight.springer.com/trials/700196689?error=cookies_not_supported&code=d2cd0412-f6f1-44a7-a84d-0cf725440aec
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Zetia Doesnt Enhance Zocor - WSJZetia Doesnt Enhance Zocor - WSJ
The long-delayed and much-speculated-about data from Merck and Schering-Ploughs Enhance study comparing whether a combination of Zetia and Zocor works better than Zocor alone were finally released today. Bottom line: Zetia, or ezetimibe generically, didnt bring anything important to the cholesterol party. Thats bound to be a bummer for sales of Zetia and Vytorin, the drug that combines Zocor, now sold generically as simvastatin, and ezetimibe.. The telling detail: there was no statistically significant difference in the primary endpoint of the study, a marker of atherosclerotic changes in the arteries called intima-media thickness, according to a Schering-Plough press release. Important secondary endpoints, the fallbacks for worried study designers, also showed no statistical difference between treatment groups.. The results of this two-year-long trial of 720 people with heterozygous familial hypercholesterolemia (HeFH), a rare, inherited form of high cholesterol that affects about 0.2% of ...
https://www.wsj.com/articles/BL-HEB-1805
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Ezetimibe interferes with the gastrointestinal absorption not only of cholesterol, but also of other molecular entities that could conceivably affect the growth of cancer cells. The fact that the combined data from all three trials showed an increase in cancer mortality with ezetimibe should not be assumed to be a chance finding until further data are in. It is appropriate that SHARP and IMPROVE-IT continue. Careful follow-up of the patients in these trials will be essential, and other existing data sets on ezetimibe-treated patients should be analyzed for cancer end points. The Food and Drug Administration has already announced that during the next few months it will conduct its own analysis of the potential cancer hazard of ezetimibe ...
http://pi-bill-articles.blogspot.com/2008/09/ezetimibe-and-cancer-uncertain.html
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In March 2008, I had the honor of participating on a panel with Drs Joseph Messer, Rick Nishimura, and Patrick OGara, all exemplary clinicians and teachers, to discuss the results of the Ezetimibe and Simvastatin in Hypercholesterolemia Enhances Atherosclerosis Regression (ENHANCE) trial at the American College of Cardiology annual Scientific Session. The meeting was full of expectation for this trial, which compared the effect of simvastatin plus ezetimibe with simvastatin alone on the progression of carotid artery intima-media thickness. Anticipation was intensified because of the controversy that accompanied delays in the publication of the trial results.1 Our panel had early access to the results and discussed the findings. When our discussions led to a consensus of opinion, we decided to present a single statement rather than 4 distinct views. I was asked to draft the statement, which was discussed and approved by the panel, and present it at the Scientific Session.. ENHANCE, presented at ...
http://circoutcomes.ahajournals.org/content/3/6/565.full?sid=4be87cfd-a76e-4ae5-8709-7aae26bac45c
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Use of a controversial new cholesterol-lowering drug, ezetimibe (trade names: Zetia, Ezetrol, Vytorin), has increased in the United States, far beyond that seen in Canada, where direct-to-consumer advertising (DTCA) is prohibited and there is more government regulation of drug reimbursement in publicly-funded drug formularies. Worldwide sales for ezetimibe is estimated at $5 billion in 2007.. A new study from Western University of Health Sciences in Pomona, Calif., in partnership with Ontario, Canadas Institute for Clinical Evaluative Sciences (ICES) and Yale University in Connecticut, found that over a recent four-year period, yearly prescriptions for ezetimibe in the U.S. grew to more than 33 million, while in Canada, with one-tenth of the U.S. population, ezetimibe only grew to 824,000 prescriptions. In 2006, ezetimibe accounted for 15 percent of all cholesterol-lowering prescriptions in the United States, while in Canada, it only represented 3.4 percent.. The study Use of Ezetimibe in the ...
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Effect of ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia: a prospective,...Effect of ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia: a prospective,...
BACKGROUND: Despite the established efficacy of statins, many patients do not achieve recommended LDL cholesterol (LDL-C) goals. Contributing factors may be inadequate dosing, increased risk for adverse effects with high-dose monotherapy, and increased potential for intolerance and adverse effects with combinations of available agents.. METHODS AND RESULTS: In a double-blind study, 628 patients with baseline LDL-C 145 to 250 mg/dL and triglycerides , or =350 mg/dL were randomly assigned to receive 1 of the following for 12 weeks: ezetimibe (10 mg/d); atorvastatin (10, 20, 40, or 80 mg/d); ezetimibe (10 mg) plus atorvastatin (10, 20, 40, or 80 mg/d); or placebo. The primary efficacy end point was percentage reduction in LDL-C for pooled ezetimibe plus atorvastatin versus pooled atorvastatin treatment groups. Ezetimibe plus atorvastatin significantly improved LDL-C, HDL cholesterol (HDL-C), triglycerides, total cholesterol:HDL-C, and high-sensitivity C-reactive protein (hs-CRP) compared with ...
https://read.qxmd.com/read/12719279/effect-of-ezetimibe-coadministered-with-atorvastatin-in-628-patients-with-primary-hypercholesterolemia-a-prospective-randomized-double-blind-trial
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NPC1L1 inhibitor ezetimibe is a reliable therapeutic agent for non-obese patients with nonalcoholic fatty liver disease<...
TY - JOUR. T1 - NPC1L1 inhibitor ezetimibe is a reliable therapeutic agent for non-obese patients with nonalcoholic fatty liver disease. AU - Enjoji, Munechika. AU - MacHida, Kazuyuki. AU - Kohjima, Motoyuki. AU - Kato, Masaki. AU - Kotoh, Kazuhiro. AU - Matsunaga, Kazuhisa. AU - Nakashima, Manabu. AU - Nakamuta, Makoto. PY - 2010/12/1. Y1 - 2010/12/1. N2 - Background: We recently examined the distribution of abdominal fat, dietary intake and biochemical data in patients with nonalcoholic fatty liver disease (NAFLD) and found that non-obese NAFLD patients did not necessarily exhibit insulin resistance and/or dysregulated secretion of adipocytokines. However, dietary cholesterol intake was superabundant in non-obese patients compared with obese patients, although total energy and carbohydrate intake was not excessive. Therefore, excess cholesterol intake appears to be one of the main factors associated with NAFLD development and liver injury. Methods. We reviewed a year of follow-up data of ...
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Statin and Ezetimibe Combination Therapy Decreases Mean Platelet Volume Compared to Statin MonotherapyStatin and Ezetimibe Combination Therapy Decreases Mean Platelet Volume Compared to Statin Monotherapy
Dear Sir:. When platelets are activated, they increase in size and change from a quiescent disc to a swollen sphere. Large platelets are more reactive and likely aggregate more than small ones [1]. Mean platelet volume (MPV), an indicator of platelet size and activation, has been shown to predict ischemic stroke, myocardial infarction, and overall vascular mortality [2,3]. The IMProved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVEIT) study showed that ezetimibe added to statin therapy further decreases low density lipoprotein cholesterol (LDL-C) levels and prevented acute coronary syndromes [4]. In this study, we investigated the lowering effect of LDL-C and MPV changes in patients who are on statin-ezetimibe combination therapy and those who receive statin monotherapy.. Patients with acute ischemic cerebral infarctions (n=120) were divided into those who were on statin therapy (n=60) and those on statin plus ezetimibe (n=60). The statin group received either atorvastatin ...
http://j-stroke.org/journal/view.php?viewtype=pubreader&number=170
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AIM: Patients with a recent myocardial infarction have an increased risk of recurrent ischaemic events. In the ESTEEM trial, the oral direct thrombin inhibitor ximelagatran reduced the risk of new ischaemic events when compared with placebo in aspirin treated post myocardial infarction patients. Ximelagatran persistently reduced markers of coagulation activity, i.e. prothrombin fragment 1 + 2 (F1 + 2) and D-dimer levels. The aim of this substudy was to evaluate the levels of these markers and activated thromboplastin time (APTT) in relation to new ischaemic events or bleeding. METHODS AND RESULTS: In the substudy, 518 out of 1883 patients were included and within 14 days after a myocardial infarction randomized to ximelagatran or placebo for 6 months. The clinical endpoints death, myocardial infarction, severe recurrent ischaemia, ischaemic stroke, and bleeding were evaluated. The levels of F1 + 2, D-dimer, and APTT were analysed at randomization and in serial samples during the study. ...
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Recent dyslipidemia guidelines for patients with diabetes mellitusRecent dyslipidemia guidelines for patients with diabetes mellitus
While the latest guidelines have recommended only statin-based treatments, ezetimibe, a drug that inhibits cholesterol absorption from the small intestine, has been introduced to the market. Ezetimibe lowers cholesterol in the blood by blocking Niemann-Pick C1-like 1 proteins, which are responsible for absorbing cholesterol in the pericytes of the small intestine wall and in hepatocytes, thereby enabling cholesterol to be excreted in the stool [12]. The IMProved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT), which examined the effect of ezetimibe in 18,144 patients with acute coronary syndrome, compared the incidence of cardiovascular diseases between a simvastatin 40 mg/ezetimibe 10 mg group and a simvastatin 40 mg group [13]. After 6 years of follow-up, the mean LDL-C concentration at the end of the study was 53.7 mg/dL in the simvastatin/ezetimibe group and 69.5 mg/dL in the simvastatin group. This result demonstrated that the additional administration of ezetimibe ...
https://www.pfmjournal.org/journal/view.php?number=83
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study: a patient treated with atorvastatin, 20 mg/d, died of Ezetimibe/simvastatin reduced LDL-C levels by more than chronic obstructive pulmonary disease (not considered 50% from baseline at these doses, fulfilling the ADA rec- ommendation of a 30% to 40% reduction from baseline.2 Laboratory adverse events occurred in 8 patients (1.6%) This study also confirmed the superior attainment of LDL- in the ezetimibe/simvastatin group and 10 patients (1.4%) C levels of less than 70 mg/dL in high-risk patients with in the atorvastatin group. Drug-related LAEs occurred in 3 ezetimibe/simvastatin vs atorvastatin and did so across a patients in both treatment assignments. No serious LAEs wider range of dosages than previously reported.20 Thus, occurred, and no patients discontinued study participation these results add to the clinical experience with ezetimibe/ simvastatin, affirming its effectiveness in the management No patient had a creatine kinase elevation 10 or more of high LDL-C levels11-13,20,21 ...
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Ezetimibe/simvastatin is commonly prescribed to treat high cholesterol and triglycerides. This eMedTV resource describes how the medication works, explains when and how to take it, lists some of its potential side effects, and more.
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Effects of fluvastatin extended-release (80 mg) alone and in combination with ezetimibe (10 mg) on low-density lipoprotein...Effects of fluvastatin extended-release (80 mg) alone and in combination with ezetimibe (10 mg) on low-density lipoprotein...
BACKGROUND: Combining lipid-lowering agents with complementary mechanisms of action can provide greater cholesterol reductions than using either agent alone, improving achievement of target low-density lipoprotein cholesterol (LDL-C) levels.. OBJECTIVES: The aim of this study was to assess the effects of fluvastatin extended-release (XL) 80 mg/d administered alone or combined with ezetimibe 10 mg/d on plasma lipid levels and inflammatory parameters in patients with primary hypercholesterolemia. The tolerability of both regimens was also evaluated.. METHODS: In this multicenter, randomized, open-label, parallel-group study, patients with hypercholesterolemia were randomized in a 1:1 ratio to receive fluvastatin XL 80 mg/d alone or in combination with ezetimibe 10 mg/d for 12 weeks. The primary end point was the percentage change from baseline to week 12 in LDL-C level with fluvastatin XL + ezetimibe combination therapy compared with fluvastatin XL alone. Plasma concentrations of inflammatory ...
https://read.qxmd.com/read/18343245/effects-of-fluvastatin-extended-release-80-mg-alone-and-in-combination-with-ezetimibe-10-mg-on-low-density-lipoprotein-cholesterol-and-inflammatory-parameters-in-patients-with-primary-hypercholesterolemia-a-12-week-multicenter-randomized-open-label-parallel
Lipitor (atorvastatin) vs. Vytorin (simvastatin & ezetimibe)Lipitor (atorvastatin) vs. Vytorin (simvastatin & ezetimibe)
Lipitor (atorvastatin) and Vytorin (simvastatin and ezetimibe) are used to lower cholesterol levels in the blood. Lipitor and Vytorin contain HMG-CoA reductase inhibitors (
https://www.medicinenet.com/lipitor_atorvastatin_vs_vytorin_simvastatin_ezetim/article.htm
Simvastatin With or Without Ezetimibe in Familial Hypercholesterolemia - American College of CardiologySimvastatin With or Without Ezetimibe in Familial Hypercholesterolemia - American College of Cardiology
The results of the multicenter, randomized ENHANCE trial seem to suggest that in patients with very high baseline LDL levels, such as those with HeFH, the combination of ezetimibe/simvastatin 10/80 mg does not result in significant changes in the mean carotid IMT at 2 years when compared with high-dose simvastatin 80 mg alone. There was also no difference in the incidence of cardiovascular mortality, nonfatal myocardial infarction, nonfatal stroke, and need for revascularization, although this study was not powered to study clinical outcomes. The incidence of adverse events was similar. The LDL-lowering effect of ezetimibe/simvastatin was greater than that achieved with high-dose simvastatin alone ...
http://www.acc.org/latest-in-cardiology/clinical-trials/2010/02/23/19/05/enhancenbsp8212nbsppresented-at-scaiacc-i2-summitacc-2008
Efficacy and Safety of Coadministration of Ezetimibe and Simvastatin in Adolescents With Heterozygous Familial...Efficacy and Safety of Coadministration of Ezetimibe and Simvastatin in Adolescents With Heterozygous Familial...
We show that, consistent with studies of ezetimibe coadministration with simvastatin in adults, significant incremental decreases of approximately 15% in LDL-C levels compared with administration of simvastatin alone were achieved within 6 weeks of treatment. These decreases were sustained throughout the subsequent 26-week, double-blind phase of the study in adolescent subjects with HeFH. Prolonged reductions were maintained through 53 weeks in the overall study population. Significantly greater reductions from baseline in total cholesterol, non-HDL-C, and apo B levels were also documented after 6 weeks and again at 33 weeks in subjects who received coadministration of ezetimibe with simvastatin compared with simvastatin monotherapy. These parameters also remained at reduced levels throughout the final 20-week phase of the study.. Mean incremental LDL-C reductions associated with coadministration of ezetimibe were consistent across the 10-, 20-, and 40-mg simvastatin dosing groups after 6 weeks ...
http://www.onlinejacc.org/content/52/17/1421
Modulation of hyperglycemia and oxidative stress by Ezetimibe in Sreptozotocin induce diabetes mellitus rats
Diabetes mellitus (DM) is metabolic diseases characterized by chronic hyperglycemia due to reducing in insulin secretion, insulin function, or both. Ezetimibe is a drug that lowers plasma cholesterol levels. A total of 18 male adult albino rats were used in this study. The animals randomized into 3 groups (of 6 rats each). Rats in first group were injected with citrate buffer only and used as healthy control group. While the rats in other two groups were injected with streptozotocin (STZ) at a dose of 60 mg/kg I.P. and treated as following (for 12 weeks), diabetic control group rats received no treatment. Ezetimibe treated group rats received Ezetimibe 6 mg/kg orally once daily. Every 2 weeks, blood glucose level is measured. At the end of 12th weeks, blood samples were collected to measure the blood glucose level and superoxide dismutase activity, and then the animals were sacrificed. The pancreas was removed for histopathology assessment for the degree of islets damage. In result, Ezetimibe was
https://kphrs.uokerbala.edu.iq/article_91686.html
Fixed-Dose Combos of Ezetimibe/Rosuvastatin Best Rosuvastatin Monotherapy in Primary Hypercholesterolemia - MPRFixed-Dose Combos of Ezetimibe/Rosuvastatin Best Rosuvastatin Monotherapy in Primary Hypercholesterolemia - MPR
For patients with primary hypercholesterolemia, fixed-dose combination of ezetimibe plus rosuvastatin is more effective than rosuvastatin alone
https://www.empr.com/medical-news/fixed-dose-combos-of-ezetimiberosuvastatin-best-rosuvastatin-monotherapy-in-primary-hypercholesterolemia/article/519031/
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Ran-Ezetimibe - Uses, Side Effects, Interactions - MedBroadcast.comRan-Ezetimibe - Uses, Side Effects, Interactions - MedBroadcast.com
Ran-Ezetimibe: Ezetimibe belongs to the group of medications known as cholesterol absorption inhibitors. It lowers cholesterol levels by decreasing the bodys ability to absorb cholesterol from the digestive system. It is used in addition to exercise and a healthy diet to lower cholesterol levels for people with high cholesterol. It may also be used with additional cholesterol-lowering medications known as statins or fenofibrate when either therapy alone is not sufficient to reduce cholesterol to desired levels.
https://medbroadcast.com/drug/getdrug/ran-ezetimibe
Simvastatin + Ezetimibe பயன்பாடுகள், மருந்தளவு, பக்க விளைவுகள், நன்மைகள், தொடர்புகள் மற்றும் எச்சரிக்கைகள்Simvastatin + Ezetimibe பயன்பாடுகள், மருந்தளவு, பக்க விளைவுகள், நன்மைகள், தொடர்புகள் மற்றும் எச்சரிக்கைகள்
Simvastatin + Ezetimibe-ன் பயன்பாடுகள், மருந்தளவு, பக்க விளைவுகள், நன்மைகள், தொடர்புகள் மற்றும் எச்சரிக்கைகள் ஆகியவற்றை கண்டுபிடியுங்கள்.
https://www.myupchar.com/ta/medicine/simvastatin-ezetimibe-p37143002
A green, chemoselective, and practical approach toward N-(2-azetidinonyl) 2,5-disubstituted pyrroles - RSC Advances (RSC...A green, chemoselective, and practical approach toward N-(2-azetidinonyl) 2,5-disubstituted pyrroles - RSC Advances (RSC...
Pyrrole and 2-azetidinone are two essential heterocyclic scaffolds, which are being broadly used in medicinal chemistry and drug discovery field. A green and practical method to synthesize novel N-(2-azetidinonyl) 2,5-disubstituted pyrroles, which are comprised of both pyrrole and 2-azetidinone moieties, has
https://pubs.rsc.org/en/Content/ArticleLanding/2013/RA/C3RA42266F
2-[<sup>18</sup>F]F-A-85380: A PET radioligand for α<sub>4</sub>β<sub>2</sub>...
TY - JOUR. T1 - 2-[18F]F-A-85380. T2 - A PET radioligand for α4β2 nicotinic acetylcholine receptors. AU - Chefer, Svetlana I.. AU - Horti, Andrew G.. AU - Koren, Andrei O.. AU - Gündisch, Daniela. AU - Links, Jonathan M.. AU - Kurian, Varughese. AU - Dannals, Robert F.. AU - Mukhin, Alexey G.. AU - London, Edythe D.. PY - 1999/9/9. Y1 - 1999/9/9. N2 - 2-[18F]FLUORO-3-(2(S)-AZETIDINYLMETHOXY)PYRIDINE (2[18F]F-A-85380), a ligand for nicotinic acetylcholine receptors (nAChRs) was evaluated in an in vitro binding assay with membranes of rat brain and in vivo by PET in Rhesus monkey brain. The ligand has high affinity for α4β2 nAChRs (K(D) = 50 pM), crosses the blood-brain barrier, and distributes in the monkey brain in a pattern consistent with that of α4β2 nAChRs. The specific/non- specific binding ratio increased steadily, reaching a value of 3.3 in the thalamus at 4 h. The specific binding of 2-[18F]F-A-85380 was reversed by cytisine. These results, in combination with the data ...
https://jhu.pure.elsevier.com/en/publications/2-sup18supff-a-85380-a-pet-radioligand-for-%CE%B1sub4sub%CE%B2sub2sub-nicot
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Ezetimibe for primary hypercholesterolemia | CochraneEzetimibe for primary hypercholesterolemia | Cochrane
Colantonio L, Cermignani E, Ciapponi A, Calcagno JI. Ezetimibe for primary hypercholesterolemia. Cochrane Database of Systematic Reviews 2015, Issue 6. Art. No.: CD006298. DOI: 10.1002/14651858.CD006298. ...
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Alternatives to Advicor
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http://cholesterol.emedtv.com/advicor/alternatives-to-advicor-p2.html
Cholesterol - Real Life PharmacologyCholesterol - Real Life Pharmacology
Subscribe: Apple Podcasts , Google Podcasts , Stitcher , RSS , More. On this episode, I discuss ezetimibe pharmacology. Ezetimibe works by inhibiting Niemann-Pick C1-Like1 (NPC1L1) transporter. This transporter aids in cholesterol absorption so by blocking it, we can reduce cholesterol levels (and LDL) in the bloodstream.. Ezetimibe is usually very well tolerated. Diarrhea, myopathy, and elevations in LFTs are adverse effects that have been reported but do not occur at high rates.. Ezetimibe is dosed at 10 mg once daily. This is a nice advantage because this is a starting dose and the usual treatment dose.. With the most recent cholesterol guideline updates, I do expect ezetimibe to be utilized a little more than it used to be. They place more emphasis on a target LDL and getting patients to goal.. Statins are going to be used first line for cholesterol and ezetimibe will be an add on therapy to consider. They dont, unfortunately, lower cholesterol as much as high-intensity statins do.. Be ...
https://www.reallifepharmacology.com/category/cholesterol/
Zetia please... - Forum on Managing Side Effects of HIV Treatment - TheBody.comZetia please... - Forum on Managing Side Effects of HIV Treatment - TheBody.com
Zetia has been reported to safely result in a modest further reduction of triglyceride levels in HIV+ patients in your situation. The ACTG has a Zetia study that is fully enrolled with results...
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Vytorin (Ezetimibe/Simvastatin) is used for reducing total cholesterol, LDL cholesterol, and triglycerides and for increasing HDL cholesterol. buy cheap vytorin
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Before taking ezetimibe/simvastatin, tell your doctor or pharmacist if you think you are allergic to it; or to other drugs called statins; or if you have any other allergies. This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: active liver disease. Before using this medication, tell your doctor or pharmacist your medical history, especially of: heart disease, history of liver disease, kidney disease, underactive thyroid (hypothyroidism), poorly controlled diabetes, alcohol use. Developing severe muscle damage, which is rare, can sometimes lead to serious kidney problems (see the Side Effects section in this handout). This medication is usually temporarily stopped if you have any condition which can increase your risk of developing kidney problems. Before you stop taking your medication, notify your doctor immediately if you have any of the following conditions: major surgery, trauma, serious ...
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http://abcnews.go.com/Health/HeartDiseaseNews/cheap-niacin-beats-pricier-zetia-heart-patients/story?id=9092855&page=2
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AziridinesAziridines
Certain 1,4-dipoles form from azetidines. N-unsubstituted aziridines can be opened with olefins in the presence of strong Lewis ...
https://en.wikipedia.org/wiki/Aziridines
Fatty acid amide hydrolaseFatty acid amide hydrolase
3: tetra-substituted azetidine ureas with in vivo activity". Bioorganic & Medicinal Chemistry Letters. 22 (2): 901-6. doi: ... Surprising selectivity of chiral azetidine ureas". Bioorganic & Medicinal Chemistry Letters. 19 (15): 4241-4. doi:10.1016/j. ... "Azetidine derivatives as FAAH inhibitors", published 28 May 2013, assigned to Vernalis (R&D) Ltd. Roughley SD, Browne H, Macias ...
https://en.wikipedia.org/wiki/Fatty_acid_amide_hydrolase
LythranidineLythranidine
Pinder, A. R (1992). "Azetidine, pyrrole, pyrrolidine, piperidine, and pyridine alkaloids". Natural Product Reports. 9 (5): 491 ...
https://en.wikipedia.org/wiki/Lythranidine
Beta-lactamBeta-lactam
Azetidine Lactone Lectka enantioselective beta-lactam synthesis Gilchrist T (1987). Heterocyclic Chemistry. Harlow: Longman ...
https://en.wikipedia.org/wiki/Beta-lactam
Amine alkylationAmine alkylation
Intramolecular reactions of haloamines X-(CH2)n-NH2 give cyclic aziridines, azetidines and pyrrolidines. N-alkylation is a ... Examples of N-alkylation with alkyl halides are the syntheses of benzylaniline, 1-benzylindole, and azetidine. Another example ...
https://en.wikipedia.org/wiki/Amine_alkylation
Secondary amino acidSecondary amino acid
Azetidine-2-carboxylic acid, which is a smaller homolog of proline in plants. Proline and its higher homolog pipecolic acid ...
https://en.wikipedia.org/wiki/Secondary_amino_acid
Asymmetric addition of dialkylzinc compounds to aldehydesAsymmetric addition of dialkylzinc compounds to aldehydes
Martens and colleagues have used azetidine alcohols as ligands for asymmetric zinc additions. The researchers found that when ...
https://en.wikipedia.org/wiki/Asymmetric_addition_of_dialkylzinc_compounds_to_aldehydes
Mugineic acidMugineic acid
... is the organic compound consisting of a azetidine group and three carboxylates. A colorless solid, it is a ...
https://en.wikipedia.org/wiki/Mugineic_acid
Cannabinoid receptor antagonistCannabinoid receptor antagonist
In addition to the five and six-membered ring analogs there are other cyclic derivatives such as the azetidines. One example is ... the methylsulfonamide azetidine derivative which has a 1,1-diaryl group that mimics the 1,5-diaryl moiety of the ...
https://en.wikipedia.org/wiki/Cannabinoid_receptor_antagonist
Edward RubensteinEdward Rubenstein
Rubenstein, Edward (2008). "Misincorporation of the Proline Analogue Azetidine-2-Carboxylic Acid in the Pathogenesis of ... azetidine-2-carboxylic acid (Aze). This compound eludes the gate-keeping function of the prolyl tRNAs, and enters a wide range ...
https://en.wikipedia.org/wiki/Edward_Rubenstein
Johnson-Corey-Chaykovsky reactionJohnson-Corey-Chaykovsky reaction
With epoxides and aziridines the reaction serves as a ring-expansion to produce the corresponding oxetane or azetidine. The ...
https://en.wikipedia.org/wiki/Johnson–Corey–Chaykovsky_reaction
3,3-Diphenylcyclobutanamine3,3-Diphenylcyclobutanamine
β-Phenylmethamphetamine Fezolamine Azetidine ring variation: Carnmalm B, Rämsby S, Renyi AL, Ross SB, Ogren SO (January 1978 ...
https://en.wikipedia.org/wiki/3,3-Diphenylcyclobutanamine
Discovery and development of dipeptidyl peptidase-4 inhibitorsDiscovery and development of dipeptidyl peptidase-4 inhibitors
Azetidine-based DPP-4 inhibitors can roughly be grouped into three main subcategories: 2-cyanoazetidines, 3-fluoroazetidines, ... The most potent ketoazetidines and cyanoazetidines have large hydrophobic amino acid groups bound to the azetidine nitrogen and ... "Azetidine-Based Inhibitors of Dipeptidyl Peptidase IV (DPP IV)", Current Topics in Medicinal Chemistry, 7 (6): 597-608, doi: ... "New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors", Bioorganic & Medicinal Chemistry ...
https://en.wikipedia.org/wiki/Discovery_and_development_of_dipeptidyl_peptidase-4_inhibitors
Non-proteinogenic amino acidsNon-proteinogenic amino acids
Thialysine quisqualic acid canavanine azetidine-2-carboxylic acid cephalosporin C penicillamine Naturally-occurring cyanotoxins ... canavanine and azetidine-2-carboxylic acid.Cephalosporin C has an α-aminoadipic acid (homoglutamate) backbone that is amidated ...
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Bcr-Abl tyrosine-kinase inhibitorBcr-Abl tyrosine-kinase inhibitor
... pyrrolidine and azetidine derivatives were introduced. The most promising substance from these final modifications was labeled ...
https://en.wikipedia.org/wiki/Bcr-Abl_tyrosine-kinase_inhibitor
BafetinibBafetinib
... pyrrolidine and azetidine derivatives were introduced. The most promising substance from these final modifications was labeled ...
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TebaniclineTebanicline
A-366,833A-366,833
Azetidines, Nicotinic agonists, Nitriles, Pyridines, Pyrrolidines, Stimulants, All stub articles, Analgesic stubs). ...
https://en.wikipedia.org/wiki/A-366,833
1,3,3-Trinitroazetidine1,3,3-Trinitroazetidine
List of MeSH codes (D03)List of MeSH codes (D03)
... azetidines MeSH D03.383.082.301.100 - azetidinecarboxylic acid MeSH D03.383.097.217 - aziridines MeSH D03.383.097.217.300 - ...
https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D03)
SarolanerSarolaner
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SiponimodSiponimod
Azetidines, Lipids, Multiple sclerosis, Novartis brands, Trifluoromethyl compounds). ...
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Lysergic acid 2,4-dimethylazetidideLysergic acid 2,4-dimethylazetidide
It was developed as a rigid analog of LSD with the diethylamide group constrained into an azetidine ring in order to map the ... There are three possible stereoisomers around the azetidine ring, with the (S,S)-(+) isomer being the most active, slightly ... Azetidines, Designer drugs, Psychedelia, Serotonin receptor agonists). ...
https://en.wikipedia.org/wiki/Lysergic_acid_2,4-dimethylazetidide
DelafloxacinDelafloxacin
Azetidines, Chloroarenes, Fluoroquinolone antibiotics, Pyridines, Carboxylic acids). ...
https://en.wikipedia.org/wiki/Delafloxacin
TabtoxinTabtoxin
CobimetinibCobimetinib
Azetidines, Benzamides, Experimental cancer drugs, Fluoroarenes, Iodoarenes, MEK inhibitors, Piperidines, Protein kinase ...
https://en.wikipedia.org/wiki/Cobimetinib
AzelnidipineAzelnidipine
Azetidines, Nitrobenzenes, Isopropyl esters, All stub articles, Cardiovascular system drug stubs). ...
https://en.wikipedia.org/wiki/Azelnidipine
XimelagatranXimelagatran
Sazetidine ASazetidine A
Azetidines, Phenol ethers, Pyridines, Alkyne derivatives, Primary alcohols). ...
https://en.wikipedia.org/wiki/Sazetidine_A
BaricitinibBaricitinib
Azetidines, Breakthrough therapy, COVID-19 drug development, Non-receptor tyrosine kinase inhibitors, Pyrazoles, ...
https://en.wikipedia.org/wiki/Baricitinib
Azetidine - WikipediaAzetidine - Wikipedia
Perhaps the most abundant azetidine containing natural product is azetidine-2-carboxylic acid - a toxic mimic of proline. Azete ... Azetidine is a saturated heterocyclic organic compound containing three carbon atoms and one nitrogen atom. It is a liquid at ... Azetidines can be prepared by reduction of azetidinones (β-lactams) with lithium aluminium hydride. Even more effective is a ... It is controlled by Baldwins Rules with remarkable functional group tolerance.[citation needed] Azetidine and its derivatives ...
https://en.wikipedia.org/wiki/Azetidine
Azetidines | Harvard Catalyst Profiles | Harvard CatalystAzetidines | Harvard Catalyst Profiles | Harvard Catalyst
"Azetidines" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical Subject ... This graph shows the total number of publications written about "Azetidines" by people in Harvard Catalyst Profiles by year, ... Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold. J Med ... Below are the most recent publications written about "Azetidines" by people in Profiles. ...
https://connects.catalyst.harvard.edu/Profiles/display/Concept/Azetidines
CN104892582A - Azetidines as mek inhibitors for the treatment of proliferative diseases - Google Patents
CN104892582A - Azetidines as mek inhibitors for the treatment of proliferative diseases - Google Patents. Azetidines as mek ... 150000001539 azetidines Chemical class 0.000 title description 3 * 150000001875 compounds Chemical class 0.000 claims abstract ... QUERMGFVJPRMJL-UHFFFAOYSA-N tert-butyl azetidine-1-carboxylate Chemical class data:image/svg+xml;base64, ... GFZWHAAOIVMHOI-UHFFFAOYSA-N azetidine-3-carboxylic acid Chemical compound data:image/svg+xml;base64, ...
https://patents.google.com/patent/CN104892582A/en
Cas 193269-78-2,1-Boc-3-(Amino)azetidine | lookchemCas 193269-78-2,1-Boc-3-(Amino)azetidine | lookchem
We also Provide Trading Suppliers & Manufacture for 193269-78-2 1-Boc-3-(Amino)azetidine. ... CAS DataBase Reference: 1-Boc-3-(Amino)azetidine(CAS DataBase Reference). *NIST Chemistry Reference: 1-Boc-3-(Amino)azetidine( ... 1-Boc-3-(Amino)azetidine. Cas No: 193269-78-2. No Data. 1 Metric Ton. 100 Metric Ton/Day. Shanghai AngewChem Co., Ltd.. Contact ... 1-Boc-3-(Amino)azetidine. Cas No: 193269-78-2. No Data. 10 Milligram. Amadis Chemical Co., Ltd.. Contact Supplier ...
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Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors - Open Research OnlineAzetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors - Open Research Online
Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.. Journal of Medicinal Chemistry, 51(6 ... Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors ... A new class of inhibitors 4-oxo-β-lactams (azetidine-2,4-diones), containing the required structural elements for molecular ...
http://oro.open.ac.uk/10817/
Fmoc-azetidine-3-carboxylic acid | CAS 193693-64-0 | P212121 Store
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Azetidines | Products - 001CHEMICALAzetidines | Products - 001CHEMICAL
tert-butyl 3-hydroxy-3-(2-methyl-1-nitro-propyl)azetidine-1-carboxylate ...
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DI-fusion Synthesis of the proline analogue [2,3 3H]azetidine 2...
Synthesis of the proline analogue [2,3 3H]azetidine 2 carboxylic acid: Uptake and incorporation in Arabidopsis thaliana and ... Synthesis of the proline analogue [2,3 3H]azetidine 2 carboxylic acid: Uptake and incorporation in Arabidopsis thaliana and ...
https://difusion.ulb.ac.be/vufind/Record/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/123934/Details
2-Bromoacetophenone|3-Amino-1-Boc-azetidine|ChonTech
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1016731-24-0 | MFCD07772065 | 1-Cbz-3-(aminomethyl)azetidine
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897019-61-3 | 3-(ethoxymethyl)azetidine;hydrochloride | C6H14ClNO897019-61-3 | 3-(ethoxymethyl)azetidine;hydrochloride | C6H14ClNO
... azetidine;hydrochloride, CAS number 897019-61-3, Molecular Formula C6H14ClNO. ...
https://www.keyorganics.net/3-ethoxymethylazetidine-hydrochloride-897019-61-3-c6h14clno.html
Identification of n-substituted triazolo-azetidines as novel antibacterials using pdualrep2 HTS platform | CoLabIdentification of n-substituted triazolo-azetidines as novel antibacterials using pdualrep2 HTS platform | CoLab
Conclusion: N-substituted triazolo-azetidine scaffold may be used as a versatile starting point for the development of novel ... HTS rounds and rescreen campaign have revealed the antibacterial activity of a series of Nsubstituted triazolo-azetidines and ... N-substituted triazolo-azetidine scaffold may be used as a versatile starting point for the development of novel active and ... HTS rounds and rescreen campaign have revealed the antibacterial activity of a series of Nsubstituted triazolo-azetidines and ...
https://colab.ws/articles/10.2174/1386207322666190412165316
CAS: 1133116-29-6 - 1-[(3-Bromophenyl)sulfonyl]azetidineCAS: 1133116-29-6 - 1-[(3-Bromophenyl)sulfonyl]azetidine
Safety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 studySafety and activity of RRx-001 in patients with advanced cancer: a first-in-human, open-label, dose-escalation phase 1 study
Azetidines / administration & dosage* * Azetidines / adverse effects * Azetidines / pharmacokinetics * Dose-Response ...
https://pubmed.ncbi.nlm.nih.gov/26296952/
Cas Number 436087-09-1|1-(2-AMINO-PHENYL)-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER|C17H20N2O2 | molecularinfo.comCas Number 436087-09-1|1-(2-AMINO-PHENYL)-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER|C17H20N2O2 | molecularinfo.com
AZETIDINE-3-CARBOXYLICACIDMETHYLESTER;Formulanor is C17H20N2O2;Synonyms ;More Molecular information Lookup with Cas No on ... 1-(2-AMINO-PHENYL)-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER. Cas No,Cas Number,CAS Registry Number:436087-09-1 .. Chemical Name, ... Tags: 1-(2-AMINO-PHENYL)-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER, 436087-09-1, C17H20N2O2, CAS 436087-09-1, CAS NO 436087-09-1, ... Molecular Name:1-(2-AMINO-PHENYL)-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER Formulanor:C17H20N2O2 Synonyms: Molecular Weight: ...
https://www.molecularinfo.com/cas-no-database/436087-09-1/
Nicotinic alpha4beta2 receptor binding in dementia with Lewy bodies using 123I-5IA-85380 SPECT demonstrates a link between...Nicotinic alpha4beta2 receptor binding in dementia with Lewy bodies using 123I-5IA-85380 SPECT demonstrates a link between...
Azetidines * Butanones * Female * Hallucinations / diagnostic imaging* * Hallucinations / metabolism * Hallucinations / ...
https://pubmed.ncbi.nlm.nih.gov/18295510/?dopt=Abstract
Registration Dossier - ECHARegistration Dossier - ECHA
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
https://echa.europa.eu/registration-dossier/-/registered-dossier/4046/4/14
Inhibition of Plasmodium falciparum phenylalanine tRNA synthetase provides opportunity for antimalarial drug development:...Inhibition of Plasmodium falciparum phenylalanine tRNA synthetase provides opportunity for antimalarial drug development:...
Bicyclic azetidine compounds possess antimalarial activity via targeting of the cytoplasmic Plasmodium falciparum (Pf) protein ... Here we present the co-crystal structure of PfcFRS with a potent inhibitor, the bicyclic azetidine BRD7929. Our studies reveal ... Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase. ...
https://www.cell.com/structure/fulltext/S0969-2126
Molecules | Free Full-Text | Xanthines Studied via Femtosecond Fluorescence SpectroscopyMolecules | Free Full-Text | Xanthines Studied via Femtosecond Fluorescence Spectroscopy
Stereoselective Fluorescence Quenching in the Electron Transfer Photooxidation of Nucleobase-Related Azetidines by ...
https://www.mdpi.com/1420-3049/21/12/1668
Vauthey Research Group - Group MembersVauthey Research Group - Group Members
Hip to be square: Building brighter fluorophores with azetidine Org.: NCCR Chemical Biology ...
http://www.unige.ch/sciences/chifi/Vauthey/seminars.php?lang=en&yr=2014&wid=1&nocolors=&dept=chior&pres=list
Vauthey Research Group - Group MembersVauthey Research Group - Group Members
Hip to be square: Building brighter fluorophores with azetidine Org.: NCCR Chemical Biology ...
http://www.unige.ch/sciences/chifi/Vauthey/seminars.php?lang=en&yr=2014&wid=1&nocolors=&dept=all&pres=list
Focus Synthesis - R&D Chemicals - Page 25
Boc-azetidine-3-carboxylic acid *Molecular Formula: C9H15NO4 ...
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Combi-BlocksCombi-Blocks
3-(Methoxymethyl)azetidine. Purity: 97%. [942400-33-1], MFCD16556179. QB-6358. 3-(Methoxymethyl)-azetidine trifluoroacetate. ...
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1,2,4-oxadiazoles (including Hydrogenated) Patents and Patent Applications (Class 548/131) - Justia Patents Search1,2,4-oxadiazoles (including Hydrogenated) Patents and Patent Applications (Class 548/131) - Justia Patents Search
Abstract: The present invention relates to substituted pyrazole azetidines, processes for preparing them, pharmaceutical ... Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical ...
https://patents.justia.com/patents-by-us-classification/548/131
DESCARTES, MENDEL-2, RUTHERFORD-2 Trials Look at Impacts of Evolocumab - American College of CardiologyDESCARTES, MENDEL-2, RUTHERFORD-2 Trials Look at Impacts of Evolocumab - American College of Cardiology
Keywords: Pyrroles, Azetidines, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Risk Factors, Heptanoic Acids, ...
https://www.acc.org/Latest-in-Cardiology/Articles/2014/03/28/14/41/Evolocumab
Registration Dossier - ECHARegistration Dossier - ECHA
tert-butyl 5-(3-(3,5-dichloro-4-fluorophenyl)-4,4,4-trifluorobut-2-enoyl)-3H-spiro[azetidine-3,1-isobenzofuran]-1- ...
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Cas 52-90-4,L-Cysteine | lookchemCas 52-90-4,L-Cysteine | lookchem
2S,4R)-N-allyloxycarbonyl-2-cyano-4-methyl-azetidine 1240490-42-9 C12H16N2O4S ...
https://www.lookchem.com/casno52-90-4.html
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Synthonix, Inc | Building BlocksSynthonix, Inc | Building Blocks
Terrorists try changes after Snowden leaks, official says - CNN Security Clearance - CNN.com BlogsTerrorists try changes after Snowden leaks, official says - CNN Security Clearance - CNN.com Blogs
1 BOC Azetidine 3 carboxylic acid 98 процентов купить онлайн Интернет магазин ХИММЕД. Tegs: 1 BOC 4 Piperidinecarboxaldehyde 95 ...
https://security.blogs.cnn.com/2013/06/25/terrorists-try-changes-after-snowden-leaks-official-says/comment-page-3/?replytocom=2280385
BicyclicCompoundsDerivativeInhibitorsScaffoldAcidSynthesisPotentAminoCitationSeriesDrugAntimalarial activityDerivativesProlineRingsDisplaysSynthesisMethylChiralDerivativesAziridinesBicyclic azetidinesTert-butoxycarbonylProline analogueInhibitorsTrifluoromethylReductive2018AcidCompoundProductStudiesManufacturersCurrentUniversityType
Bicyclic4
  • Bicyclic azetidine compounds possess antimalarial activity via targeting of the cytoplasmic Plasmodium falciparum ( Pf ) protein translation enzyme phenylalanine-tRNA synthetase (cFRS). (cell.com)
  • Here we present the co-crystal structure of Pf cFRS with a potent inhibitor, the bicyclic azetidine BRD7929. (cell.com)
  • The inhibition of Plasmodium cytosolic phenylalanine tRNA-synthetase (cFRS) by a novel series of bicyclic azetidines has shown the potential to prevent malaria transmission, provide prophylaxis, and offer single-dose cure in animal models of malaria. (diamond.ac.uk)
  • To date, however, the molecular basis of Plasmodium cFRS inhibition by bicyclic azetidines has remained unknown. (diamond.ac.uk)
Compounds2
  • N-substituted triazolo-azetidine scaffold may be used as a versatile starting point for the development of novel active and selective antibacterial compounds. (colab.ws)
  • Novel potent azetidine-based compounds irreversibly inhibit Stat3 activation and induce antitumor response against human breast tumor growth in vivo. (sbpdiscovery.org)
Derivative2
  • An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. (childrensmercy.org)
  • In their publication, the authors describe a new anti-TB drug termed BRD4592 (a derivative of Azetidine ) that kills the TB bacterium by allosteric inhibition of the enzyme tryptophan synthase - required for production of the amino acid tryptophan which is used for making proteins. (nature.com)
Inhibitors1
  • A new class of inhibitors 4-oxo-β-lactams (azetidine-2,4-diones), containing the required structural elements for molecular recognition, inhibit porcine pancreatic elastase (PPE) but show a dramatically lower reactivity toward hydroxide compared with the analogous inhibitors 3-oxo-β-sultams. (open.ac.uk)
Scaffold1
  • Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold. (harvard.edu)
Acid12
  • Perhaps the most abundant azetidine containing natural product is azetidine-2-carboxylic acid - a toxic mimic of proline. (wikipedia.org)
  • Click the button below to add the Fmoc-azetidine-3-carboxylic acid 1 g to your wish list. (p212121.com)
  • In the scholarly research of Compact L-Azetidine-2-carboxylic acid disc276 in cutaneous melanoma, researchers discovered that MiR-29c appearance could inversely regulate Compact disc276 appearance (14). (icics2010.org)
  • ILT4 is one of the immunoglobulin-like very family members that inhibit immune system cell L-Azetidine-2-carboxylic acid function (37). (icics2010.org)
  • The up-regulation of Compact disc276 L-Azetidine-2-carboxylic acid pursuing PBK-overexpression could possibly be reversed by MSL1 depletion. (icics2010.org)
  • Mechanistically, MSL1 acts as a mediator in the PBK-MSL1-Compact disc276 L-Azetidine-2-carboxylic acid axis (39). (icics2010.org)
  • Those contradictory outcomes recommended that TLT-2 is certainly L-Azetidine-2-carboxylic acid unlikely to be always a receptor for Compact disc76, and an alternative solution receptor interacts with Compact disc276 to mediate inhibitory immune system replies. (icics2010.org)
  • Coexistence of L-azetidine 2-carboxylic acid (AzC) an inhibitor of collagen synthesis attenuated both effects of Asc 2-P in a dose-dependent manner. (one-may.com)
  • Finally, we found an important beneficious L-Azetidine-2-carboxylic acid effect of fluoxetine L-Azetidine-2-carboxylic acid or sertraline treatment on cancer progression. (edtechtraining.ca)
  • Although a direct impact of medication and tension treatment on tumor biology cannot become eliminated, the beneficial aftereffect of fluoxetine and sertraline L-Azetidine-2-carboxylic acid is apparently because of a restoration of antitumor immune response mainly. (edtechtraining.ca)
  • 104 cells of each tumor were re-suspended in RPMI culture medium without FBS, seeded into the top L-Azetidine-2-carboxylic acid well of a transwell chamber with 8.0-m pores (Jet Biofil), and allowed to migrate toward medium containing 10% of FBS for 24?h. (edtechtraining.ca)
  • In comparison to the neurons which responded to the ionophoresis of DHPG, less were activated by the selective mGluR5 agonist trans-azetidine dicarboxylic acid (t-ADA). (ox.ac.uk)
Synthesis1
  • DI-fusion Synthesis of the proline analogue [2,3 3H]azetidine 2. (ac.be)
Potent1
  • N-Nitroso-lacidipine Or diethyl (E)-4-(2-(3-(tert-butoxy)-3-oxoprop-1-en-1-yl)phenyl)-2,6-dimethyl-1-nitroso-1,4-dihydropyridine-3,5-dicarboxylate, is a highly potent new calcium antagonist of the dihydropyridine, which show long-lasting antihypertensive effects. (veeprho.com)
Amino1
  • Azetidine can also be produced by a multistep route from 3-amino-1-propanol. (wikipedia.org)
Citation1
  • citation needed] Azetidine and its derivatives are relatively rare structural motifs in natural products. (wikipedia.org)
Series1
  • HTS rounds and rescreen campaign have revealed the antibacterial activity of a series of Nsubstituted triazolo-azetidines and their isosteric derivatives that has not been reported previously. (colab.ws)
Drug1
  • In short, the fda approval of both l-theanine and l-azetidine has led to the development of a new class of prescription drug, called modafinil. (killtenrats.com)
Antimalarial activity1
  • Bicyclic azetidine compounds possess antimalarial activity via targeting of the cytoplasmic Plasmodium falciparum (Pf) protein translation enzyme phenylalanine-tRNA synthetase (cFRS). (diamond.ac.uk)
Derivatives1
  • 1-azirine 3-position acetic acid adduct aldehyde alkaloids alkene alkyl amine anhydride aromatic azetidine aziridine azirine base basic benzene benzene ring benzo benzofuran bond Bromination carbon atoms carbonyl CH3 CH3 Chem Chemical Reactions Chemistry chloride condensation COOC2H5 COOCH3 COOH cyclization cycloaddition derivatives diaziridine 3/5(6). (pandudesign.com)
Proline1
  • Metabolic pulse-labeling studies of cells recovering from either heat-shock treatment, exposure to sodium arsenite, or exposure to an amino acid analogue of proline, L-azetidine 2-carboxylic acid, revealed interesting differences with respect to the individual stress proteins produced, their kinetics of induction, as well as the decay in their synthesis during the recovery period. (rupress.org)
Rings1
  • We recently discovered a general method to improve the properties of classic fluorophores by replacing N,N-dimethylamino groups with four-membered azetidine rings to create the "Janelia Fluor" dyes. (janelia.org)
Displays1
  • A CNN' metallocyclic complex was prepared by oxidative addition of palladium(0) to an ortho bromo 2,4-cis-disubstituted azetidine and its crystal structure displays a slightly pyramidalized metal-ligand orientation. (elsevier.com)
Synthesis6
  • A TfOH-catalyzed highly efficient synthesis of biologically active ( E )-2-cyanoacrylamides and 3-substituted azetidine-2,4-diones has been reported with 64-94% yields under metal-free conditions. (rsc.org)
  • 2. Azetidine synthesis project. (europa.eu)
  • Synthesis of azetidines and pyrrolidines: towards medicinal chemistry and organocatalysis applications. (bham.ac.uk)
  • disulfiram is an inhibitor of RA synthase, 2,2'-dipyridyl and azetidine-2-carboxylic acid are inhibitors of collagen synthesis. (elsevier.com)
  • 16. Synthesis and Sar Studies on Azetidine-Containing Dipeptides as Hcmv Inhibitors . (nih.gov)
  • Synthesis and Antimicrobial Screening of Some 4-Substituted-3-Chloro-2-Oxo-Azetidine Derivatives. (ajrconline.org)
Methyl1
  • Silver catalyzed 1,3-dipolar cycloaddition reactions between methyl 2-(oxetane/azetidine-3 ylidene) acetate as dipolarophiles and imines derived from -amino acid methyl esters, 2-aminomethyl pyridine and 2-aminomethyl pyrazine afforded oxetane/azetidine containing spirocycles in 40-77% yield. (whiterose.ac.uk)
Chiral4
  • In the second year, a Pd(II)-catalyzed γ-C-H amination process was developed, in which a series of cyclic secondary alkyl amines are converted into highly substituted chiral drug-like azetidines. (europa.eu)
  • The novel chiral azetidine derivatives are currently under biological evaluation. (europa.eu)
  • The chiral ketene generated from commercially available l-(+)-diethyl tartrate on Staudinger cycloaddition with different imines gave spiro-β-lactams in good yields.These spiro-β-lactams were transformed into azetidine-2,3-diones in excellent yields in a two-step process. (mab-bauprojekte.ch)
  • I will first describe how my laboratory will use chiral organocatalysts that function through enamine and iminium activation of aldehydes to develop methods of preparing chiral biologically relevant scaffolds, beginning with chiral azetidines. (123holdings.sg)
Derivatives1
  • A new series of 2-oxo-azetidine derivatives of isoniazid have been synthesized and evaluated for their Anti-bacterial, Antifungal and Anti-tubercular activity. (ajrconline.org)
Aziridines1
  • This research involves the study of regio- and stereoselective ring transformations of constrained (phosphonylated) azaheterocycles such as aziridines, azetidines and beta-lactams. (ugent.be)
Bicyclic azetidines7
  • The compounds, called bicyclic azetidines, specifically target an enzyme responsible for protein production within the parasite, the authors report in the journal Science Translational Medicine . (brightsurf.com)
  • After looking at many classes of anti-microbial compounds, they determined that the anti-malarial bicyclic azetidines was a candidate and tested them against Cryptosporidium. (brightsurf.com)
  • They found that the bicyclic azetidines targeted an enzyme that makes transfer RNA, the molecule that carries amino acids when the cell makes proteins. (brightsurf.com)
  • The paper "Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase" is available online. (brightsurf.com)
  • Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase. (mindzilla.com)
  • Prior studies in also have highlighted the strength of bicyclic azetidines that inhibit parasite phenylalanine-tRNA synthetases (PheRS) (16), recommending these may possess broad-spectrum activity against other apicomplexans also. (ilgazozveren.com)
  • In keeping with this prediction, latest studies reveal that bicyclic azetidines may also be powerful inhibitors of development (17). (ilgazozveren.com)
Tert-butoxycarbonyl2
  • Order Liverpool ChiroChem's (2S,3S)-1-(tert-butoxycarbonyl)-3-(4-fluorophenyl)azetidine-2-carboxylic acid. (zageno.com)
  • 2S,3S)-1-(tert-butoxycarbonyl)-3-(4-fluorophenyl)azetidine-2-carboxylic acid. (zageno.com)
Proline analogue2
  • We previously isolated mutants resistant to the proline analogue azetidine-2-carboxylate derived from a diploid sake yeast strain. (omicsdi.org)
  • Wild type Saccharomyces cerevisiae cells (S228C background) were treated with 1 mg/ml of the proline analogue azetidine-2-carboxylic acid (AZC) for 30 and 90 minutes. (ucsd.edu)
Inhibitors1
  • 6. Discovery of Novel Azetidine Amides as Potent Small-Molecule STAT3 Inhibitors. (nih.gov)
Trifluoromethyl1
  • Sarolaner is a member of the isoxazoline class of parasiticides and the chemical name is 1-(5'-((5S)-5-(3,5-Dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)-3'-H-spiro(azetidine-3,1'-(2)benzofuran)-1-yl)-2-(methylsulfonyl)ethanone. (nih.gov)
Reductive2
  • Cyclization of the amine to displace the γ-tosylate completes the formal C-N reductive elimination process to azetidine. (europa.eu)
  • For product 2, if you go for the intramolecular route then the product of a reductive amination should be azetidine. (stackexchange.com)
20181
  • The global market size of 1-Fmoc-3-carboxymethyl-azetidine is $XX million in 2018 with XX CAGR from 2014 to 2018, and it is expected to reach $XX million by the end of 2024 with a CAGR of XX% from 2019 to 2024. (search4research.com)
Acid3
  • We also provide, for the first time, high-resolution structures of globular proteins containing pipecolic acid, azetidine-2-carboxylic acid and 3,4 dehydroproline in the polypeptide chain. (caltech.edu)
  • Leete Edward, Louters Laurence L., Prakash Rao H.S.: Biosynthesis of azetidine-2-carboxylic acid in Convallaria majalis: Studies with N-15 labelled precursors. (cas.cz)
  • Azetidine-2-carboxylic acid reduced the size of cartilages, without causing remarkable malformation. (elsevier.com)
Compound1
  • Chip uses this compound to prepare poly(azetidine) in Dr. Paul Rupar's group. (ua.edu)
Product2
  • We were surprised to find, however, that reaction produced only the γ-C-H acetoxylation product, with no sign of azetidine, when treated under identical conditions to the aziridine forming process. (europa.eu)
  • Maybe at best you can get a mixture of the azetidine with the open chain product and possibly oligo/polymerisation products, a mess. (stackexchange.com)
Studies1
  • In light of these preliminary computational studies, we re-evaluated our design hypothesis for azetidine formation. (europa.eu)
Manufacturers1
  • 1.The report provides key statistics on the market status of the 1-Fmoc-3-carboxymethyl-azetidine manufacturers and is a valuable source of guidance and direction for companies and individuals interested in the industry. (search4research.com)
Current1
  • Global 1-Fmoc-3-carboxymethyl-azetidine Market Report 2019 - Market Size, Share, Price, Trend and Forecast is a professional and in-depth study on the current state of the global 1-Fmoc-3-carboxymethyl-azetidine industry. (search4research.com)
University1
  • In the 2000s, a team led by David E. Nichols at Purdue University set to develop a rigid analog of LSD with the diethylamide group constrained into an azetidine ring in order to map the binding site at the 5-HT 2A receptor . (psychonautwiki.org)
Type1
  • Notably, the proper choice of base and solvent are critical to the desired oxetane formation , in that the use of potassium tert -butoxide in THF leads to selective Grob-type fragmentation to produce the 3-methylene azetidine 34 instead. (organic-chemistry.org)
Azetidines | Harvard Catalyst Profiles | Harvard Catalyst
Azetidines | Harvard Catalyst Profiles | Harvard Catalyst (connects.catalyst.harvard.edu)
Molecules | Free Full-Text | Xanthines Studied via Femtosecond Fluorescence Spectroscopy
Molecules | Free Full-Text | Xanthines Studied via Femtosecond Fluorescence Spectroscopy (mdpi.com)
Identification of n-substituted triazolo-azetidines as novel antibacterials using pdualrep2 HTS platform | CoLab
Identification of n-substituted triazolo-azetidines as novel antibacterials using pdualrep2 HTS platform | CoLab (colab.ws)
Uncategorized Archives - Anzap Web
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FERNANDO ARTEAGA ARTEAGA (Institute for the Advancement of Higher Education International Education and Research Division) |...
FERNANDO ARTEAGA ARTEAGA (Institute for the Advancement of Higher Education International Education and Research Division) |... (researchers.general.hokudai.ac.jp)
Kudos - Dr Leonardo Degennaro - Public Profile
Kudos - Dr Leonardo Degennaro - Public Profile (growkudos.com)
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Paragenesis of Palladium-Cobalt Nanoparticle in Nitrogen-Rich Carbon Nanotubes as a Bifunctional Electrocatalyst for Hydrogen...
Paragenesis of Palladium-Cobalt Nanoparticle in Nitrogen-Rich Carbon Nanotubes as a Bifunctional Electrocatalyst for Hydrogen... (americanelements.com)
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A rapid deposition of polydopamine coatings induced by iron (III) chloride/hydrogen peroxide for loose nanofiltration. |...
A rapid deposition of polydopamine coatings induced by iron (III) chloride/hydrogen peroxide for loose nanofiltration. |... (americanelements.com)
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CAS 1306-24-7 | AMERICAN ELEMENTS ®
CAS 1306-24-7 | AMERICAN ELEMENTS ® (americanelements.com)
Nitrogen doped carbon quantum dots mediated silver phosphate/bismuth vanadate Z-scheme photocatalyst for enhanced antibiotic...
Nitrogen doped carbon quantum dots mediated silver phosphate/bismuth vanadate Z-scheme photocatalyst for enhanced antibiotic... (americanelements.com)
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Synthesis and Characterization of Silicon/Reduced Graphene Oxide Composites as Anodes for Lithium Secondary Batteries. |...
Synthesis and Characterization of Silicon/Reduced Graphene Oxide Composites as Anodes for Lithium Secondary Batteries. |... (americanelements.com)
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Control of the optical properties of cadmium selenide nanoparticles using magadiite. | AMERICAN ELEMENTS ®
Control of the optical properties of cadmium selenide nanoparticles using magadiite. | AMERICAN ELEMENTS ® (americanelements.com)
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Molybdenum (Mo) | AMERICAN ELEMENTS ®
Molybdenum (Mo) | AMERICAN ELEMENTS ® (americanelements.com)
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CAS 1188507-66-5 | AMERICAN ELEMENTS ®
CAS 1188507-66-5 | AMERICAN ELEMENTS ® (americanelements.com)
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