OrganismsChemicals and DrugsPhenomena and Processes
Azabicyclo CompoundsOctanesBicyclo Compounds, HeterocyclicQuinuclidinesTropanesBicyclo CompoundsHydrocarbons, CyclicHexanesHeterocyclic Compounds, 2-RingCyclooctanesOctanolsAza Compoundsalpha7 Nicotinic Acetylcholine ReceptorTrypanosoma brucei rhodesienseStereoisomerismReceptors, NicotinicNicotinic AgonistsMolecular StructureMolecular ConformationPyridines
Azabicyclo Compounds
Bicyclic bridged compounds that contain a nitrogen which has three bonds. The nomenclature indicates the number of atoms in each path around the rings, such as [2.2.2] for three equal length paths. Some members are TROPANES and BETA LACTAMS.
Octanes
Eight-carbon saturated hydrocarbon group of the methane series. Include isomers and derivatives.
Bicyclo Compounds, Heterocyclic
A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)
Quinuclidines
Tropanes
N-methyl-8-azabicyclo[3.2.1]octanes best known for the ones found in PLANTS.
Bicyclo Compounds
Hydrocarbons, Cyclic
Organic compounds composed exclusively of carbon and hydrogen forming a closed ring that may be either alicyclic or aromatic.
Hexanes
Six-carbon saturated hydrocarbon group of the methane series. Include isomers and derivatives. Various polyneuropathies are caused by hexane poisoning.
Heterocyclic Compounds, 2-Ring
A class of organic compounds containing two ring structures, one of which is made up of more than one kind of atom, usually carbon plus another atom. The heterocycle may be either aromatic or nonaromatic.
Cyclooctanes
A group of compounds with an 8-carbon ring. They may be saturated or unsaturated.
Octanols
Isomeric forms and derivatives of octanol (C8H17OH).
Aza Compounds
alpha7 Nicotinic Acetylcholine Receptor
A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.
Trypanosoma brucei rhodesiense
A hemoflagellate subspecies of parasitic protozoa that causes Rhodesian sleeping sickness in humans. It is carried by Glossina pallidipes, G. morsitans and occasionally other species of game-attacking tsetse flies.
Stereoisomerism
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Receptors, Nicotinic
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Nicotinic Agonists
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Molecular Structure
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Molecular Conformation
The characteristic three-dimensional shape of a molecule.
Pyridines
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism. (1/173)

Zopiclone is a widely prescribed, nonbenzodiazepine hypnotic that is extensively metabolized by the liver in humans. The aim of the present study was to identify the human cytochrome P-450 (CYP) isoforms involved in zopiclone metabolism in vitro. Zopiclone metabolism was studied with different human liver microsomes and a panel of heterologously expressed human CYPs (CYP1A2, 2C8, 2C9, 2C18, 2C19, 2D6, 2E1, and 3A4). In human liver microsomes, zopiclone was metabolized into N-desmethyl-zopiclone (ND-Z) and N-oxide-zopiclone (NO-Z) with the following K(m) and V(m) of 78 +/- 5 and 84 +/- 19 microM, 45 +/- 1 and 54 +/- 5 pmol/min/mg for ND-Z and NO-Z generation, respectively. Ketoconazole (CYP3A inhibitor) inhibited approximately 40% of the generation of both metabolites, sulfaphenazole (CYP2C inhibitor) inhibited the formation of ND-Z, whereas alpha-naphtoflavone (CYP1A), quinidine (CYP2D6), and chlorzoxazone (CYP2E1) did not affect zopiclone metabolism. The generation of ND-Z and NO-Z were highly correlated to testosterone 6beta-hydroxylation (CYP3A activity, r = 0.95 and 0.92, respectively; p =.0001), and ND-Z was highly correlated to CYP2C8 activity (paclitaxel 6alpha-hydroxylase; r = 0.76, p =.004). Recombinant CYP2C8 had the highest enzymatic activity toward zopiclone metabolism into both its metabolites, followed by CYP2C9 and 3A4. CYP3A4 is the major enzyme involved in zopiclone metabolism in vitro, and CYP2C8 contributes significantly to ND-Z formation.  (+info)

Zopiclone use during pregnancy. (2/173)

QUESTION: One of my patients, whom I had treated with a 2-week course of zopiclone for insomnia, conceived while using the medication. She is concerned. How should I advise her? ANSWER: Based on available, albeit limited, evidence, zopiclone does not appear to be a major human teratogen.  (+info)

Characterization of the interaction of zopiclone with gamma-aminobutyric acid type A receptors. (3/173)

Zopiclone is a cyclopyrrolone that is used clinically as a hypnotic. Although this drug is known to interact with neuronal gamma-aminobutyric acid type A receptors, its binding site(s) within the receptor oligomer has been reported to be distinct from that of the classical benzodiazepines. After photoaffinity labeling with flunitrazepam, receptors in rat cerebellar membranes showed differentially reduced affinity for flunitrazepam and zopiclone by 50- and 3-fold, respectively. Because histidine 101 of the alpha-subunit is a major site of photolabeling, we have made specific substitutions of this residue and studied the consequences on the binding properties of zopiclone and diazepam using recombinant alpha1beta2gamma2-receptors transiently expressed in tsA201 cells. Both compounds showed similar binding profiles with receptors containing mutated alpha-subunits, suggesting a similar interaction with the residue at position 101. At alpha1beta2gamma3-receptors, flunitrazepam affinity was dramatically decreased by approximately 36-fold, whereas the affinity for zopiclone was decreased only 3-fold, suggesting a differential contribution of the gamma-subunit to the binding pocket. Additionally, we used electrophysiological techniques to examine the contribution of the gamma-subunit isoform in the receptor oligomer to ligand recognition using recombinant receptors expressed in Xenopus oocytes. Both compounds are agonists at alpha1beta2gamma2- and alpha1beta2gamma3-receptors, with flunitrazepam being more potent but less efficacious. In summary, these data suggest that histidine 101 of the alpha1-subunit plays a similar role in ligand recognition for zopiclone, diazepam, and flunitrazepam.  (+info)

Mechanism-based pharmacokinetic/pharmacodynamic modeling of the electroencephalogram effects of GABAA receptor modulators: in vitro-in vivo correlations. (4/173)

A mechanism-based pharmacokinetic-pharmacodynamic (PK/PD) model for neuroactive steroids, comprising a separate characterization of 1) the receptor activation process and 2) the stimulus-response relationship, was applied to various nonsteroidal GABAA receptor modulators. The EEG effects of nine prototypical GABAA receptor modulators (six benzodiazepines, one imidazopyridine, one cyclopyrrolone, and one beta-carboline) were determined in rats in conjunction with plasma concentrations. Population PK/PD modeling revealed monophasic concentration-EEG effect relationships with large differences in potency (EC50) and intrinsic activity between the compounds. The data were analyzed on the basis of the mechanism-based PK/PD model for (synthetic) neuroactive steroids on the assumption of a single and unique stimulus-response relationship. The model converged yielding estimates of both the apparent in vivo receptor affinity (KPD) and the in vivo intrinsic efficacy (ePD). The values of KPD ranged from 0.41 +/- 0 ng.ml(-1) for bretazenil to 436 +/- 72 ng.ml(-1) for clobazam and the values for e(PD) from -0.27 +/- 0 for methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate to 0.54 +/- 0.02 for diazepam. Significant linear correlations were observed between KPD for unbound concentrations and the affinity in an in vitro receptor bioassay (r = 0.93) and between e(PD) and the GABA-shift in vitro (r = 0.95). The findings of this investigation show that the in vivo effects of nonsteroidal GABAA receptor modulators and (synthetic) neuroactive steroids can be described on the basis of a single unique transducer function. In this paradigm, the nonsteroidal GABAA receptor modulators behave as partial agonists relative to neuroactive steroids.  (+info)

Effect of zaleplon, a non-benzodiazepine hypnotic, on melatonin secretion in rabbits. (5/173)

Melatonin, a major hormone secreted by the pineal gland, is known to play an important role in regulation of the circadian rhythm. (N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide (zaleplon) is a non-benzodiazepine hypnotic that acts via the benzodiazepine site of the GABA(A) receptor. In the present study, we investigated the effect of zaleplon on melatonin secretion in rabbits using RIA and compared the effect to triazolam and zopiclone. Zaleplon increased a dose-dependent concentration of melatonin in rabbit plasma collected at 30 min after intravenous administration at doses of 1 and 2 mg/kg. The zaleplon-induced increase in plasma melatonin level was not blocked by flumazenil, a benzodiazepine-receptor antagonist. In contrast, triazolam and zopiclone failed to affect the plasma melatonin level. We also investigated the effect of zaleplon on intracellular cAMP in rat pinealocytes. Consequently, zaleplon had no effect on the intracellular cAMP levels in rat pinealocytes. These results of the present studies suggest that zaleplon may promote melatonin secretion and the elevation of plasma levels of melatonin may suggest an influence of zaleplon on chronobiology.  (+info)

Dependence on legal psychotropic drugs among alcoholics. (6/173)

AIMS: Dependence on legal psychotropic drugs (PTD) has been reported to have increased in alcoholics, but previous studies report conflicting results concerning the rate of increase and clinical characteristics. The aim of the present study was first, to assess the dependence rate of PTD among alcoholics in open and institutionalized care, and to compare these populations with the general population, and second, to assess rates and doses of high- and low-dose PTD-dependence among alcoholics. METHODS: In 1997, alcoholics in open and institutionalized care were asked to anonymously fill in a questionnaire on their drug use and dependence. Healthy controls were included. The number of attending subjects was 130 open-care alcoholics at the Department of Alcohol and Drug Diseases in Malmo, Sweden; 23 alcoholics in institutionalized care at Karlsvik Rehabilitation Centre in Hoor, Sweden; and 120 healthy controls at Vardcentralen Kirseberg, a primary health care centre located in a Malmo area. The approximate attendance rate was 75, 70 and 95%, respectively. The questionnaire was based on DSM-IV criteria for dependence. RESULTS: The total rate of PTD-dependent alcoholics was higher in the institutionalized group (35%) than in the open-care setting (14%): difference in proportions (p(1)-p(2) 21%; 95% CI: 1%, 41%). Alcoholics were more often PTD-dependent (17%) than were healthy controls (2%), (p(1)-p(2) 15%; 95% CI: 9%, 21%). Benzodiazepines (BZD) were the most common PTD. Only four out of a total of 23 BZD-dependent alcoholics developed high-dose BZD-dependence. Those subjects were also misusing other drugs, including cannabis. CONCLUSIONS: We conclude that alcoholism is associated with legal PTD-dependence and illegal drug misuse. High-dose BZD-dependence is infrequent among BZD-dependent alcoholics.  (+info)

Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats. (7/173)

The encephalographic (EEG) properties of zaleplon were investigated in comparison with those of other sedative hypnotics in conscious rats with chronically implanted electrodes. The oral administration of zaleplon (0.25-1.0 mg/kg), triazolam (0.0625-0.25 mg/kg), zopiclone (1.0-4.0 mg/kg), brotizolam (0.0625-0.25 mg/kg), and nitrazepam (0.125-0.5 mg/kg) lengthened the total sleep in a dose-dependent manner. On distribution of sleep-wakefulness stages, zaleplon, in particular, increased the slow wave deep sleep (SWDS), whereas triazolam, brotizolam, and nitrazepam increased the slow wave light sleep (SWLS) in a dose-dependent manner. Zopiclone significantly increased the SWDS at a dose of 2 mg/kg and both the SWLS and the SWDS at a dose of 4 mg/kg. All tested hypnotics caused no influence on fast wave sleep (FWS) at doses tested. The appearance of the sleep-inducing activity of zaleplon was more rapid than those of any compounds tested, and zaleplon significantly increased the relative EEG power density in the delta frequency band over that of triazolam at 20 and 30 min after the administration in the spectral analysis. Therefore, the present findings suggest that the non-benzodiazepine zaleplon can be expected to exhibit high practical potential as a hypnotic and is characterized by an increase in SWDS with rapid onset of hypnotic action.  (+info)

Characterization of two novel N-methyl-D-aspartate antagonists: EAA-090 (2-[8,9-dioxo-2,6-diazabicyclo [5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride). (8/173)

Two novel N-methyl-d-aspartate (NMDA) antagonists with unique chemical structures, EAA-090 (2-[8,9-dioxo-2, 6-diazabicyclo[5.2.0]non-1(7)-en2-yl]ethylphosphonic acid) and EAB-318 (R-alpha-amino-5-chloro-1-(phosphonomethyl)-1H-benzimidazole-2-propanoic acid hydrochloride), were compared with CGS-19755 (Selfotel) in ligand binding, electrophysiology, and neuroprotection assays. CGS-19755, EAA-090 and EAB-318 inhibited [(3)H]3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid binding to NMDA receptors with IC(50) values of 55, 28, and 7.9 nM, respectively. All three compounds decreased the duration of spontaneous synaptic currents and inhibited NMDA-activated currents in rat hippocampal neurons. IC(50) values for inhibition of current induced by 10 microM NMDA were 795, 477, and 69 nM for CGS-19755, EAA-090, and EAB-318, respectively. The NMDA antagonists protected chick embryo retina slices and cultured rat hippocampal and cortical neurons from glutamate- and NMDA-induced neurotoxicity. In experiments in which different NMDA receptor splice variants and subtypes were expressed in Xenopus oocytes, all three antagonists preferentially blocked NMDA-elicited currents mediated by N-methyl-d-aspartate receptor (NR)1 splice variants containing the N-terminal insertion. They also favored NR2A-versus NR2B- or NR2C-containing NMDA receptors, with EAA-090 showing the greatest selectivity. EAA-090 was 10 times more potent at blocking NR2A-versus NR2B- or NR2C-containing NMDA receptors. In addition to being the most potent NMDA antagonist, EAB-318 inhibited alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and kainate receptors. The combination of NMDA and AMPA/kainate block enabled EAB-318 to protect neurons against ischemia induced cell death.  (+info)

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DailyMed - ESZOPICLONE tablet, film coatedDailyMed - ESZOPICLONE tablet, film coated
The pharmacokinetics of eszopiclone have been investigated in healthy subjects (adult and elderly) and in patients with hepatic disease or renal disease. In healthy subjects, the pharmacokinetic profile was examined after single doses of up to 7.5 mg and after once-daily administration of 1, 3, and 6 mg for 7 days. Eszopiclone is rapidly absorbed, with a time to peak concentration (tmax) of approximately 1 hour and a terminal-phase elimination half-life (t1/2) of approximately 6 hours. In healthy adults, eszopiclone does not accumulate with once-daily administration, and its exposure is dose-proportional over the range of 1 to 6 mg.. Absorption and Distribution Eszopiclone is rapidly absorbed following oral administration. Peak plasma concentrations are achieved within approximately 1 hour after oral administration. Eszopiclone is weakly bound to plasma protein (52 to 59%). The large free fraction suggests that eszopiclone disposition should not be affected by drug-drug interactions caused by ...
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=48925d07-1e06-4761-bbdc-d8b7e70ad155
Effectiveness of non-benzodiazepine hypnotics in treatment of adult insomnia: meta-analysis of data submitted to the Food and...
Objectives To investigate the effectiveness of non-benzodiazepine hypnotics (Z drugs) and associated placebo responses in adults and to evaluate potential moderators of effectiveness in a dataset used to approve these drugs.. Design Systematic review and meta-analysis.. Data source US Food and Drug Administration (FDA).. Study selection Randomised double blind parallel placebo controlled trials of currently approved Z drugs (eszopiclone, zaleplon, and zolpidem).. Data extraction Change score from baseline to post-test for drug and placebo groups; drug efficacy analysed as the difference of both change scores. Weighted raw and standardised mean differences with their confidence intervals under random effects assumptions for polysomnographic and subjective sleep latency, as primary outcomes. Secondary outcomes included waking after sleep onset, number of awakenings, total sleep time, sleep efficiency, and subjective sleep quality. Weighted least square regression analysis was used to explain ...
https://www.bmj.com/content/345/bmj.e8343.abstract
DailyMed - ESZOPICLONE tablet, film coatedDailyMed - ESZOPICLONE tablet, film coated
The effect of eszopiclone on reducing sleep latency and improving sleep maintenance was established in studies with 2100 subjects (ages 18 to 86) with chronic and transient insomnia in six placebo-controlled trials of up to 6 months duration. Two of these trials were in elderly patients (n=523). Overall, at the recommended adult dose (2 to 3 mg) and elderly dose (1 to 2 mg), eszopiclone significantly decreased sleep latency and improved measures of sleep maintenance (objectively measured as wake time after sleep onset [WASO] and subjectively measured as total sleep time).. 14.1 Transient Insomnia. Healthy adults were evaluated in a model of transient insomnia (n=436) in a sleep laboratory in a double-blind, parallel-group, single-night trial comparing two doses of eszopiclone and placebo. Eszopiclone 3 mg was superior to placebo on measures of sleep latency and sleep maintenance, including polysomnographic (PSG) parameters of latency to persistent sleep (LPS) and WASO.. 14.2 Chronic Insomnia ...
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=2cedcc9d-ab83-3b5a-e054-00144ff8d46c&audience=consumer
The β-lactamase inhibitor avibactam (NXL104) does not induce ampC | IDRThe β-lactamase inhibitor avibactam (NXL104) does not induce ampC | IDR
The β-lactamase inhibitor avibactam (NXL104) does not induce ampC β -lactamase in Enterobacter cloacae Christine Miossec, Monique Claudon, Premavathy Levasseur, Michael T Black Novexel, Romainville, France Abstract: Induction of ampC β-lactamase expression can often compromise antibiotic treatment and is triggered by several β-lactams (such as cefoxitin and imipenem) and by the β-lactamase inhibitor clavulanic acid. The novel β-lactamase inhibitor avibactam (NXL104) is a potent inhibitor of both class A and class C enzymes. The potential of avibactam for induction of ampC expression in Enterobacter cloacae was investigated by ampC messenger ribonucleic acid quantitation. Cefoxitin and clavulanic acid were confirmed as ampC inducers, whereas avibactam was found to exert no effect on ampC expression. Thus, avibactam is unlikely to diminish the activity of any partner β-lactam antibiotic against AmpC-producing organisms. Keywords: β-lactamase, ampC, induction, NXL104, avibactam
https://www.dovepress.com/the-beta-lactamase-inhibitor-avibactam-nxl104-does-not-induce-ampc-bet-peer-reviewed-article-IDR
Zimovane (Zopiclone Zopitin) 7.5 mgZimovane (Zopiclone Zopitin) 7.5 mg
|p align=justify||strong|How does it work?|/strong||br| Zimovane contains the active ingredient |em||strong|zopiclone|/strong||/em|, which is a type of medicine called a non-benzodiazepine hypnotic. It acts in the brain to aid sleep. |/p| |br| |p align=justify|Zopiclone works by acting on receptors in the brain called GABA receptors. This causes the release of a neurotransmitter called GABA in the brain.|/p| |br| |p align=justify|GABA is a neurotransmitter that acts as a natural nerve-calming agent. It helps keep the nerve activity in the brain in balance, and is involved in inducing sleepiness, reducing anxiety and relaxing muscles.|/p| |br| |p align=justify|Zopiclone can be used as a short-term treatment for insomnia. This includes difficulty falling asleep, waking in the night, waking early in the morning, sleeping problems related to psychiatric disorders and sleeping problems that are causing severe distress.|/p| |br| |p align=justify|Zopiclone decreases the time taken
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6-Month Chronic Efficacy & Safety Study of Eszopiclone in Adult Subjects With Primary Insomnia - Full Text View -...6-Month Chronic Efficacy & Safety Study of Eszopiclone in Adult Subjects With Primary Insomnia - Full Text View -...
This is a double blind, randomized (2:1; eszopiclone : placebo), placebo-controlled, multicenter, study of eszopiclone in subjects with primary insomnia. The study will involve up to 9 visits and subject participation will be approximately 224 days. After meeting all screening criteria, subjects will be randomized to either eszopiclone 3 mg QD or placebo. This study was previously posted by Sepracor Inc. In October 2009, Sepracor Inc. was acquired by Dainippon Sumitomo Pharma., and in October 2010, Sepracor Incs name was changed to Sunovion Pharmaceuticals Inc ...
https://clinicaltrials.gov/ct2/show/NCT00352144
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Pivotal Phase III studies evaluating the prospect of the investigational antibiotic.
Ceftazidime-avibactam is being developed with Astra Zeneca jointly. Forest Laboratories LLC., a subsidiary of Actavis plc, holds the rights to commercialize ceftazidime-avibactam in North America, while AstraZeneca holds the privileges to commercialize ceftazdime-avibactam in the rest of the global world.. Actavis reports excellent results from ceftazidime-avibactam Phase III studies in cIAI patients Actavis plc today confirmed positive topline results from RECLAIM-1 and -2, pivotal Phase III studies evaluating the prospect of the investigational antibiotic, ceftazidime-avibactam as a treatment for adult hospitalized sufferers with complicated intra-abdominal infections. Ceftazidime-avibactam includes a cephalosporin , an established treatment for significant bacterial infections, and a next generation non-beta lactam beta-lactamase inhibitor .This system appears to be more essential than those earlier described for prolonged stimulation by dopamine, as would be the case in those with ...
http://www.randbmed.com/pain-management/pivotal-phase-iii-studies-evaluating-the-prospect-of-the-investigational-antibiotic/
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Abstract: <i>In Vitro</i> and <i>In Vivo</i> Activity of Single and Dual Antimicrobial Agents Against KPC-producing <i...Abstract: <i>In Vitro</i> and <i>In Vivo</i> Activity of Single and Dual Antimicrobial Agents Against KPC-producing <i...
Background: Options for treatment of infections due to KPC-producing K. pneumoniae are limited, and combination therapy is often recommended. In this report, the in vitro and in vivo activity of potential therapeutic agents and combinations was assessed against four KPC-producing K. pneumoniae isolates. Methods: Using clinically-relevant concentrations, time-kill experiments and the Galleria mellonella model of infection were used to examine the activity of polymyxin B, ceftazidime-avibactam, meropenem, rifampin, and amikacin alone and in combination. Four isolates of KPC-producing K. pneumoniae were studied, including two isolates that were resistant to polymyxin B and had ceftazidime-avibactam MICs of 8 µg/ml. The other two K. pneumoniae isolates were susceptible to polymyxin B and had lower MICs of ceftazidime-avibactam. Results: Two isolates that were resistant to polymyxin B and with ceftazidime-avibactam MICs of 8 µg/ml were also resistant to amikacin and meropenem. When ...
https://idsa.confex.com/idsa/2017/webprogram/Paper63579.html
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Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health. These factors may affect how you should use this medication.. Alcohol use: The use of zopiclone after consuming alcohol increases the risk of severe side effects such as breathing difficulty and performing activities while not being aware or awake. Alcohol should not be consumed if you are taking zopiclone.. Anxiety or restlessness: An increase in daytime anxiety or restlessness has been observed during treatment with zopiclone.. Bad taste in mouth: Zopiclone may cause you to have a coated tongue, bad breath, or a bitter taste in your mouth. These effects often occur when this medication is being used.. Behaviour changes: This medication may worsen symptoms of depression, including thoughts of suicide or wanting to harm others. It may also cause ...
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Antimicrobial activity of ceftazidime-avibactam, ceftolozane-tazobactam and comparators tested against Pseudomonas aeruginosa...Antimicrobial activity of ceftazidime-avibactam, ceftolozane-tazobactam and comparators tested against Pseudomonas aeruginosa...
Antimicrobial activity of ceftazidime-avibactam, ceftolozane-tazobactam and comparators tested against Pseudomonas aeruginosa and Klebsiella pneumoniae isolates from United States medical centers in 2016-2018. by Sader HS, Carvalhaes CG, Streit JM, Doyle TB and Castanheira M. published in Microb. Drug Resist.: in press, 2020.. View publication. ...
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[Source: Antimicrobial Agents and Chemotherapy, full page: (LINK). Abstract, edited.] Antimicrobial Activity of Ceftazidime-Avibactam When Tested against Gram-negative Bacteria Isolated from Patients Hospitalized with Pneumonia in United States Medical Centers (2011-2015) Helio S. Sader⇑, Mariana Castanheira and Robert K. Flamm Author Affiliations: JMI Laboratories, North Liberty, Iowa, USA ABSTRACT Bacterial isolates were collected from patients…
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Eszopiclone treatment for insomnia: Effect size comparisons in patients with primary insomnia and insomnia with medical and...
TY - JOUR. T1 - Eszopiclone treatment for insomnia. T2 - Effect size comparisons in patients with primary insomnia and insomnia with medical and psychiatric comorbidity. AU - Krystal, Andrew D.. AU - McCall, W. Vaughn. AU - Fava, Maurizio. AU - Joffe, Hadine. AU - Soares, Claudio N.. AU - Huang, Holly. AU - Grinell, Todd. AU - Zummo, Jacqueline. AU - Spalding, William. AU - Marshall, Randall. PY - 2012/12/1. Y1 - 2012/12/1. N2 - Objective: The purpose of this post hoc analysis was to compare the treatment effect size of eszopiclone 3 mg for insomnia in patients with a diagnosis of primary insomnia and in several of the psychiatric and medical conditions that are most commonly comorbid with insomnia. Method: Data were analyzed from 5 large, multicenter, randomized, double-blind, placebo-controlled studies of adult outpatients of at least 1 month duration published between 2006 and 2009. Diary-derived indices of sleep and daytime functioning and the Insomnia Severity Index were compared for ...
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Much research demonstrates that benzodiazepines (BDZs) provide fast initial relief of anxiety symptoms, but evidence suggests that their effects do not differ significantly from those obtained with a placebo after 4 to 6 weeks of treatment. Also, BDZs primarily reduce somatic symptoms more than psychic symptoms (i.e. apprehension, dread, worry),. In studies involving head-to-head comparisons, medication tends to initially relieve symptoms faster than CBT, but the benefits end once patients stop taking the drug. In contrast, the benefits of CBT become more apparent with time. For example, one study compared CBT alone with the combination of CBT and zolpidem (non-benzodiazepine hypnotic). At the six-week mark, patients in both groups improved, but those who received combination treatment improved faster, sleeping an average of 20 minutes longer per night than those assigned to CBT alone. However, in the second, longer-term phase of the study, benefits of drug therapy faded. After initially ...
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1,5-Diazabicyclo[4.3.0]non-5-ene (DBN) is a chemical compound with the formula C7H12N2.[1] It is an amidine base used in organic synthesis. A related compound with related functions is 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). The relatively complex nature of the formal names for DBU and DBN (hence the common use of acronyms) reflects the fact that these compounds are bicyclic and contain several functional groups. ...
https://en.m.wikipedia.org/wiki/1,5-Diazabicyclo
USF Health News Dr. Yu Chen receives USF Excellence in Innovation Award - USF Health NewsUSF Health News Dr. Yu Chen receives USF Excellence in Innovation Award - USF Health News
The award recognizes Dr. Chen for his patented technology of novel beta-lactamase inhibitors licensed by Gordian Biotechnologies to tackle the growing problem of antibiotic resistance, for the development of collaborations with Achaogen Inc., and for his publications last year in the Journal of Medicinal Chemistry and Future Medicinal Chemistry.. Dr. Chens structure-based drug design approach has led to the development of novel small molecule inhibitors against multiple proteins involved in antibiotic resistance, metastatic cancer and Alzheimers disease. Using an interdisciplinary approach, he combines both computational and experimental techniques to investigate the function and inhibition of enzymes related to bacterial cell wall synthesis, the biological process targeted by antibiotics such as penicillin.. Dr. Chen has extensive experience in biochemistry, X-ray crystallography and molecular docking. He has characterized the catalytic mechanisms of three enzymes and determined about 40 ...
https://hscweb3.hsc.usf.edu/blog/2015/08/12/dr-yu-chen-receives-usf-excellence-in-innovation-award/
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Antibiotics - The Perfect Storm: AstraZeneca is Cutting and Running!Antibiotics - The Perfect Storm: AstraZeneca is Cutting and Running!
For the past two years I have been warning that AstraZeneca would be giving up on antibiotic research and development. Well, that day is arriving. It looks like they will continue with their submission for market approval of ceftazidime-avibactam - but what comes after that is still unclear. I have been able to confirm that AZ has told its antibiotics researchers that they should make efforts to find other jobs in the near future. Even though there has been no official announcement yet that the antibiotics research group will be disbanded, their scientists are starting to head for the hills. As far as antibiotic discovery and development goes, this has to be the most disappointing news of the entire antibiotic era. AZ has the strongest antibiotic pipeline in the industry and has an active and successful discovery effort. To jettison all this in spite of everything that has occurred in terms of regulatory reform and everything that is occurring and will occur in terms of improving the antibiotic ...
https://antibiotics-theperfectstorm.blogspot.com/2014/10/astrazeneca-is-cutting-and-running.html
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M. J. ThirumalacharM. J. Thirumalachar
2000). "Synthesis of pharmaceutical compositions with lactams and .beta.-lactams/oxo thia azabicyclo compounds". US Patent No. ... 23 May 1985). "Method, compound and composition for effecting degradation of crude petroleum and petroleum products in an ...
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MorphanMorphan
... is a chemical compound. It is the base of the benzomorphan family of drugs. Benzomorphan Azocine Morphinan Ginsburg, ... David (1950). "The synthesis of morphan (2-azabicyclo[3.3.1]nonane)". Journal of Organic Chemistry. 15 (5): 1003-5. doi:10.1021 ...
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Curtin-Hammett principleCurtin-Hammett principle
This compound is then treated with one equivalent of acyl chloride to produce the stannyl monoester. Two isomers of the stannyl ... "Quaternizations in the 8-azabicyclo[4.3.0]non-3-ene series". Journal of Organic Chemistry. 39 (3): 319-321. doi:10.1021/ ... The structure of each of the two compounds contains a twisted 16-membered macrocycle. A key step in the syntheses is selective ... P. J. Crowley; M. J. T. Robinson; M. G. Ward (1977). "Conformational effects in compounds with 6-membered rings-XII". ...
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Hofmann-Löffler reactionHofmann-Löffler reaction
... synthesis of 1-azabicyclo compounds". Chem. Commun. (16): 1168-1169. doi:10.1039/C39890001168. Hernández, R.; Medina, M.C; ... Synthesis of Chiral 7-Oxa-2-azabicyclo[2.2.1]heptane and 8-Oxa-6-azabicyclo[3.2.1]octane Ring Systems". J. Org. Chem. 68 (3): ... E. Suárez and co-workers also applied their methodology in the synthesis of chiral 8-oxa-6-azabicyclo[3.2.1]-octane 85 and 7- ... This result suggested that there is a high selectivity for the 3° hydrogen, but the intermediate tertiary chloro compound 17 is ...
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https://en.wikipedia.org/wiki/Solanaceae
Descriptor (chemistry)Descriptor (chemistry)
... the parent compound is tropine, whose systematic name is (1R, 3r, 5S)-8-methyl-8-azabicyclo[3.2.1]octane-3-ol. In this ... More generally, iso is a compound which is isomeric to the n compound (a compound in which individual atoms or atomic groups ... for cyclo this is only the case in inorganic compounds. In organic compounds, "cyclo" is frequently used as a name component, ... Here, the compounds were designated as syn configured when the aldehyde H and the O (of the oxime) or the N (of the hydrazone) ...
https://en.wikipedia.org/wiki/Descriptor_(chemistry)
List of cocaine analoguesList of cocaine analogues
Compound 7a (3′-methoxy-8-methyl-spiro(8-azabicyclo(3.2.1)octane-3,5′(4′H)-isoxazole) allosterically enhances SERT binding of ... Compounds 237a and 238a are the same compound as both are the parent for either series with a hydrogen saturated in their ... Compounds 201b & 201c were significantly more potent than cocaine while compounds 201a, 201d & 201e were significantly less ... Compounds 196k, 196n, 196o, and 197c all possess greater DAT affinity than cocaine. Compound 197b (dimethyl amide) displayed a ...
https://en.wikipedia.org/wiki/List_of_cocaine_analogues
List of phenyltropanesList of phenyltropanes
... as like upon the compounds given below. 3-Phenyl-7-azabicyclo[2.2.1]heptane derivatives Ring-contracted analogs of ... 8-azabicyclo[3.2.1]octanes and 3β-(5-Indolyl)-8-azabicyclo[3.2.1]octanes". Bioorganic & Medicinal Chemistry Letters. 11 (4): ... 3-Phenyl-9-azabicyclo[3.3.1]nonane derivatives To better elucidate the binding requirements at MAT, the methylene unit on the ... N.B. In the case of both nocaine and pethidine, N-demethyl compounds are more toxic and have a decreased seizure threshold. ...
https://en.wikipedia.org/wiki/List_of_phenyltropanes
TropaneTropane
8-Azabicyclo[3.2.1]octane (tropane without the N-methyl group) is known as nortropane or nor-tropane. Phenyltropane Tropane ... Tropane is a nitrogenous bicyclic organic compound. It is mainly known for the other alkaloids derived from it, which include ... Chemical articles with multiple compound IDs, Multiple chemicals in an infobox that need indexing, Articles without KEGG source ...
https://en.wikipedia.org/wiki/Tropane
HousaneHousane
Other methods include photolysis of 2,3-diazabicyclo[2.2.1]hept-2-ene, pyrolysis of N-Phenyl-2-oxo-3-azabicyclo[2.2.1]heptane, ... The two rings are fused in a cis configuration-this meso compound formally has (1R,4S) absolute stereochemistry. The small size ...
https://en.wikipedia.org/wiki/Housane
Alpha-4 beta-2 nicotinic receptorAlpha-4 beta-2 nicotinic receptor
... compound 2) (heterobivalent ligand: D2R agonist and nAChR antagonist) Oxantel α3β2-Nicotinic receptor α3β4-Nicotinic receptor ... 7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with ... "Bifunctional compounds targeting both D2 and non-α7 nACh receptors: Design, synthesis and pharmacological characterization". ... 7-azabicyclo[2.2.1]heptane 2-fluoro-3-(4-nitro-phenyl)deschloroepibatidine Coclaurine - alkaloid from Nelumbo nucifera ...
https://en.wikipedia.org/wiki/Alpha-4_beta-2_nicotinic_receptor
John M. Gregory (businessman)John M. Gregory (businessman)
US 5061722, Teetz, Volker; Geiger, Rolf & Urbach, Hansjorg et al., "Cis, endo-2-azabicyclo-[3.3.0]-octane-3-carboxylic acids, a ... process for their preparation, agents containing these compounds and their use", published 1991-10-29, assigned to Hoechst AG " ...
https://en.wikipedia.org/wiki/John_M._Gregory_(businessman)
Serotonin transporterSerotonin transporter
DASB compound 4b: Ki = 17 pM; 710-fold and 11,100-fold selective over DAT and NET compound (+)-12a: Ki = 180 pM at hSERT; >1000 ... Isosteres 3-cis-(3-Aminocyclopentyl)indole 8a: Ki = 220 pM allosteric modulator: 3′-Methoxy-8-methyl-spiro{8-azabicyclo[3.2.1] ... octane-3,5′(4′H)-isoxazole} (compound 7a) allosteric modulator: p-Trifluoromethyl-methcathinone The gene that encodes the ...
https://en.wikipedia.org/wiki/Serotonin_transporter
Metabotropic glutamate receptor 2Metabotropic glutamate receptor 2
Compound 1d (see reference) LY-2812223 JNJ-46356479 JNJ-40411813 GSK-1331258 Imidazo[1,2-a]pyridines 3-Aryl-5-phenoxymethyl-1,3 ... 3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: a novel series of mGluR2 positive allosteric modulators". Bioorganic & Medicinal ... 5-benzodiazepin-2-one and related compounds. MNI-137 - 8-bromo-4-(2-cyanopyridin-4-yl)-1H-benzo[b][1,4]diazepin-2(3H)-one ... 2-ones 3-(Imidazolyl methyl)-3-aza-bicyclo[3.1.0]hexan-6-yl)methyl ethers: potent, orally stable BINA: potent; modest ago- ...
https://en.wikipedia.org/wiki/Metabotropic_glutamate_receptor_2
QuinuclidoneQuinuclidone
Organic reduction of this compound gives the compound quinuclidine, structurally related to DABCO, which has one additional ... 3-Quinuclidone (1-azabicyclo[2.2.2]octan-3-one) is an uneventful molecule that can be synthesized as the hydrochloric acid salt ... Quinuclidones are a class of bicyclic organic compounds with chemical formula C7H11NO with two structural isomers for the base ... This compound rapidly reacts with water to the corresponding amino acid with a chemical half-life of 15 seconds. X-ray ...
https://en.wikipedia.org/wiki/Quinuclidone
IndolizidineIndolizidine
Catalytic synthesis of 1-azabicyclo[4.3.0]nonanes and 1-azabicyclo[5.3.0]decanes". Khimiya Geterotsiklicheskikh Soedinenii. 6: ... Indolizidine is a heterocyclic chemical compound that forms the central core of the indolizidine alkaloids such as swainsonine ...
https://en.wikipedia.org/wiki/Indolizidine
Bredts ruleBredt's rule
3. 3-Oxa-1-azabicyclo[3.3.1]nonan-2-one and 6-oxa-1-azabicyclo[3.2.1]octan-7-one, two atom-bridged bicyclic urethanes ... There has been an active research program to seek compounds inconsistent with the rule, and for bicyclic systems a limit of S ... Köbrich, Gert (1973). "Bredt Compounds and the Bredt Rule". Angew. Chem. Int. Ed. 12 (6): 464-473. doi:10.1002/anie.197304641. ... but the similar compound bicyclo[2.2.1]heptan-7-one-1-carboxylic acid remains stable beyond 500 °C, despite both being β-keto ...
https://en.wikipedia.org/wiki/Bredt's_rule
Blum-Ittah aziridine synthesisBlum-Ittah aziridine synthesis
The Blum-Ittah aziridine synthesis has been used in the synthesis of α-methylserine and 6-Azabicyclo[3.2.1]octanes. Hassner, ... Biologically Active Compounds Based on Renewable Raw Materials". European Journal of Organic Chemistry. 2003 (4): 649-659. doi: ... Pulipaka, Aravinda B.; Bergmeier, Stephen C. (2008-01-23). "A Synthesis of 6-Azabicyclo[3.2.1]octanes. The Role of N- ...
https://en.wikipedia.org/wiki/Blum–Ittah_aziridine_synthesis
BispidineBispidine
The first step includes a reaction between a compound containing acidic C-H hydrogens, an aldehyde and a primary amine, using a ... Jeyaraman, R.; Avila, S. (1981). "Chemistry of 3-Azabicyclo[3.3.1]nonanes". Chemical Reviews. 81 (2): 149-174. doi:10.1021/ ... Bispidine (3,7-diazabicyclo[3.3.1]nonane) is an organic compound that is classified as a bicyclic diamine. Although synthetic, ... compounds with tetradentate ligands based on the bispidine backbone". Journal of the Chemical Society, Dalton Transactions (23 ...
https://en.wikipedia.org/wiki/Bispidine
GSK1360707FGSK1360707F
July 2010). "6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple ... WO 2008031772, Bertani, Barbara; Di Fabio, Romano & Micheli, Fabrizio et al., "Azabicyclic compounds as inhibitors of ...
https://en.wikipedia.org/wiki/GSK1360707F
RTI-126RTI-126
The structurally related compound (-)-2β-(3-methyl-5-isoxazolyl)nortropane is a potent and selective agonist for nicotinic ... and 3-isoxazolyl-8-azabicyclo[3.2.1]octanes". Bioorganic & Medicinal Chemistry Letters. 14 (7): 1775-8. doi:10.1016/j.bmcl. ...
https://en.wikipedia.org/wiki/RTI-126
LactamLactam
2012, 112 (8), pp 4642-4686."2-Azabicyclo[2.2.1]hept-5-en-3-one: Chemical Profile of a Versatile Synthetic Building Block and ... A lactim is a cyclic carboximidic acid compound characterized by an endocyclic carbon-nitrogen double bond. They are formed ...
https://en.wikipedia.org/wiki/Lactam
IbogaineIbogaine
If the exo ethyl group on the 2-azabicyclo[2.2.2]octane system in ibogaine is replaced with an endo ethyl, then epiibogaine is ... Ibogaine and related indole compounds are susceptible to oxidation over time. The National Institute on Drug Abuse (NIDA) began ... Then, using 7-ethyl-2-azabicyclo[2.2.2]oct-5-ene and cesium carbonate in acetonitrile, the ibogaine precursor 7-ethyl-2-(2-(2- ... Ibogaine: A Novel Anti-Addictive Compound - A Comprehensive Literature Review Jonathan Freedlander, University of Maryland ...
https://en.wikipedia.org/wiki/Ibogaine
RTI-274RTI-274
Synthesis of aza-bicyclo[3.2.1]octane and aza-bicyclo[3.2.2]nonane ethers, imides, and amines". The Journal of Organic ... NS2214 appears to have been abandoned now, RTI-336 was their latest compound. RTI decided that they wanted to make all 8 ... To solve the problem of the unexpected aza-bicyclo[3.2.2]nonane rearrangement product, the original synthesis had to be ... and ligand binding of tropane ring analogs of paroxetine and an unexpected aza-bicyclo[3.2.2]nonane rearrangement product". ...
https://en.wikipedia.org/wiki/RTI-274
A-84,543A-84,543
Carreras J, Avenoza A, Busto JH, Peregrina JM (April 2007). "Synthesis of azabicyclo[2.2.n]alkane systems as analogues of 3-[1- ... 3-Pyridyl compounds, Pyrrolidines, Stimulants, All stub articles, Nervous system drug stubs). ... is widely used in scientific research into the structure and function of this receptor subtype and has been the lead compound ...
https://en.wikipedia.org/wiki/A-84,543
TC-1698TC-1698
May 2008). "Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin ... It has neuroprotective effects in animal studies, and has been used as a lead compound to find further potent derivatives. ... Marrero MB, Papke RL, Bhatti BS, Shaw S, Bencherif M (April 2004). "The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[ ... yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands". The Journal of Organic Chemistry. ...
https://en.wikipedia.org/wiki/TC-1698
Stieglitz rearrangementStieglitz rearrangement
Heesing, A.; Herdering, W. (January 1981). "Sauerstoff-insertion bei der umlagerung von 2-aza-bicyclo[2.2.1]hept-2-enderivaten ... X/1, 4th Edition: Nitro, Nitroso and Hydroxylamine Compounds (4 ed.). Georg Thieme Verlag. p. 1266. ISBN 9783131805546. Ayres, ... Application to the synthesis of heterocyclic compounds". Journal of Heterocyclic Chemistry. 33 (5): 1489-1496. doi:10.1002/jhet ...
https://en.wikipedia.org/wiki/Stieglitz_rearrangement
Insertion reactionInsertion reaction
Reed, D. D.; Bergmeier, S. C. (2007). "A Facile Synthesis of a Polyhydroxylated 2-Azabicyclo[3.2.1]octane". J. Org. Chem. 72 (3 ... Meier, H.; Zeller, K.-P. (1975). "The Wolff Rearrangement of α-Diazo Carbonyl Compounds". Angew. Chem. Int. Ed. 14 (1): 32-43. ... Ye, T.; McKervey, M. A. (1994). "Organic Synthesis with α-Diazo Carbonyl Compounds". Chem. Rev. 94 (4): 1091-1160. doi:10.1021/ ...
https://en.wikipedia.org/wiki/Insertion_reaction
Wolff-Kishner reductionWolff-Kishner reduction
Slow addition of the hydrazone is not necessary and it was found that this procedure is better suited for carbonyl compounds ... Bosch, J.; Bonjoch, J. (1981). "Synthetic route to 6-functionalized 2-azabicyclo\3.3.1]nonanes". The Journal of Organic ... Several of the presented procedures require isolation of the hydrazone compound prior to reduction. This can be complicated by ... The reactions of hydrazones and related compounds with strong bases. Part I. A modified Wolff?Kishner procedure". Journal of ...
https://en.wikipedia.org/wiki/Wolff–Kishner_reduction
CI-1017CI-1017
July 1998). "Design and synthesis of m1-selective muscarinic agonists: (R)-(−)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'- ... enantiomer of the racemic compound PD-142,505. In animals CI-1017 improves learning and memory and increases the electrical ...
https://en.wikipedia.org/wiki/CI-1017
Intramolecular reactionIntramolecular reaction
... and aza-bicyclo[2,1,1]hexanes". J. Chem. Soc. D. 19 (19): 1167. doi:10.1039/C29710001167. Corey, E. J.; Kang, M. C.; Desai, M. ... many intramolecular reactions that would not occur as an intermolecular reaction between two compounds take place. Examples of ... reactions have been used to synthesize organic compounds with interesting ring systems and topologies. For example, [2+2] ...
https://en.wikipedia.org/wiki/Intramolecular_reaction
AziridinesAziridines
... are organic compounds containing the aziridine functional group, a three-membered heterocycle with one amine (-NR-) ... "A Synthesis of 6-Azabicyclo[3.2.1]octanes. The Role of N-Substitution". J. Org. Chem. 73 (4): 1462-7. doi:10.1021/jo702444c. ... A banana bond model explains bonding in such compounds. Aziridine is less basic than acyclic aliphatic amines, with a pKa of ... The International Agency for Research on Cancer (IARC) classifies aziridine compounds as possibly carcinogenic to humans (IARC ...
https://en.wikipedia.org/wiki/Aziridines
Aza-Cope rearrangementAza-Cope rearrangement
aza-Prins-pinacol approach to 7-azabicyclo[2.2.1]heptanes and ring expansion to [3.2.1]tropanes Armstrong, A.; Shanahan, S. E. ... although other silver and copper compounds have been used. This added step allows for more precise control of iminium ion ... The example shown is a facile reaction combining a 1-aza-bicyclo[2.2.1]heptane salt starting material with paraformaldehyde at ... doi:10.1016/s0040-4039(01)86498-4. Armstrong, A.; Shanahan, S. E. (2005). "aza-Prins-pinacol approach to 7-azabicyclo[2.2.1] ...
https://en.wikipedia.org/wiki/Aza-Cope_rearrangement
EpibatidineEpibatidine
As the compound was not addictive nor did it cause habituation,[citation needed], it was initially thought to be very promising ... at α4β2 and α7 nicotinic acetylcholine receptors of new analogs of epibatidine and epiboxidine containing the 7-azabicyclo[2.2. ... the naturally occurring compound is the (+)-enantiomer; the (−)-enantiomer does not occur naturally). It was later determined ... due to challenges in conclusively identifying the compound from the limited samples collected by Daly. By the time that high- ...
https://en.wikipedia.org/wiki/Epibatidine
Mizoroki-Heck vs. Reductive HeckMizoroki-Heck vs. Reductive Heck
Cox, Caroline D.; Malpass, John R. (October 1999). "Synthesis of epibatidine isomers: Reductive Heck coupling of 2-azabicyclo[ ... In this context, developing commercially viable, efficient and sustainable synthetic routes to these compounds requires both ... deuterium-labeled compounds are accessible by using D2O in the reaction, allowing easy access to deuterated chiral oxindoles. ... δ-alkenyl carbonyl compounds were suitable substrates for the reaction; however, internal alkenes proved to be more challenging ...
https://en.wikipedia.org/wiki/Mizoroki-Heck_vs._Reductive_Heck
Mitsunobu reactionMitsunobu reaction
doi:10.1016/S0040-4039(01)81842-6. Hegedus, L. S.; Holden, M. S.; McKearin, J. M. (1984). "cis-N-TOSYL-3-METHYL-2-AZABICYCLO[ ... Tsunoda, T.; Nagino, C.; Oguri, M.; Itô, S. (1996). "Mitsunobu-type alkylation with active methine compounds". Tetrahedron ...
https://en.wikipedia.org/wiki/Mitsunobu_reaction
Organic azideOrganic azide
Chemistry of Heterocyclic Compounds: A Series Of Monographs. New York, USA: John Wiley & Sons, Inc. doi:10.1002/0471221902. ... Damon D. Reed & Stephen C. Bergmeier (2007). "A Facile Synthesis of a Polyhydroxylated 2-Azabicyclo[3.2.1]octane". J. Org. Chem ... The azo-transfer compounds, trifluoromethanesulfonyl azide and imidazole-1-sulfonyl azide react with amines to give the ... On a new class of compounds in which nitrogen is substituted for hydrogen". Proceedings of the Royal Society of London. 13: 375 ...
https://en.wikipedia.org/wiki/Organic_azide
Niphates digitalisNiphates digitalis
Compounds extracted from the pink vase sponge have been investigated for their possible use in the treatment of castration ... Smitha, Graham & Lynchb, Daneil E. (2016). "Crystal structures of three anhydrous salts of the Lewis base 1,8-di-aza-bicyclo-[ ...
https://en.wikipedia.org/wiki/Niphates_digitalis
Vince lactamVince lactam
... is the commercial name given to the bicyclic molecule γ-lactam 2-azabicyclo[2.2.1]hept-5-en-3-one. This lactam is ... Chemical articles with multiple compound IDs, Chemicals using indexlabels, Chemical articles with multiple CAS registry numbers ... 2012, 112 (8), pp 4642-4686."2-Azabicyclo[2.2.1]hept-5-en-3-one: Chemical Profile of a Versatile Synthetic Building Block and ...
https://en.wikipedia.org/wiki/Vince_lactam
AnabasineAnabasine
May 2008). "Synthesis of 2-(pyridin-3-yl)-1-azabicyclo[3.2.2]nonane, 2-(pyridin-3-yl)-1-azabicyclo[2.2.2]octane, and 2-(pyridin ... 3-Pyridyl compounds). ... 1-azabicyclo[2.2.2]octane, and 2-(Pyridin-3-yl)-1-azabicyclo[ ... made some higher potency sterically strained bicyclic analogs of anabasine: 2-(Pyridin-3-yl)-1-azabicyclo[3.2.2]nonane (TC-1698 ... yl)-1-azabicyclo[3.2.1]octane, a class of potent nicotinic acetylcholine receptor-ligands". The Journal of Organic Chemistry. ...
https://en.wikipedia.org/wiki/Anabasine
VanoxerineVanoxerine
As an example, GBR compounds are piperazine based and contain a proximal and a distal nitrogen. It was found that piperidine ... 8-azabicyclo[3.2.1]octane derivatives at monoamine transporters". Bioorganic & Medicinal Chemistry. 19 (24): 7551-8. doi: ... unlike the GBR compounds. Further SAR revealed that while there are 4 atoms connecting the two fluorophenyl rings to the ...
https://en.wikipedia.org/wiki/Vanoxerine
EpiboxidineEpiboxidine
It is used in scientific research and as a parent compound to derive newer analogues which may be safer and have greater ... Armstrong A, Bhonoah Y, Shanahan SE (October 2007). "Aza-Prins-pinacol approach to 7-azabicyclo[2.2.1]heptanes: syntheses of ... Epiboxidine is a chemical compound which acts as a partial agonist at neural nicotinic acetylcholine receptors, binding to both ... and 3-isoxazolyl-8-azabicyclo[3.2.1]octanes". Bioorganic & Medicinal Chemistry Letters. 14 (7): 1775-8. doi:10.1016/j.bmcl. ...
https://en.wikipedia.org/wiki/Epiboxidine
3-Quinuclidinyl benzilate3-Quinuclidinyl benzilate
... (QNB) (IUPAC name 1-azabicyclo[2.2.2]octan-3-yl hydroxy(diphenyl)acetate; US Army code EA-2277; NATO ... BZ is listed as a Schedule 2 compound by the OPCW (Szinicz, 2005). Edgewood Arsenal human experiments EA-3167 EA-3443 EA-3580 ...
https://en.wikipedia.org/wiki/3-Quinuclidinyl_benzilate
US9611261B2 - Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use ...
The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions ... The compounds have a general Formula I: wherein variables A 4 , A 5 , A 6 , A 8 , each of R a , R b , R 1 , R 2 , R 3 and R 7 ... The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods ... The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. ...
https://patents.google.com/patent/US9611261/en
3Z,4S)-N-{[3-(3-Methoxyphenyl)-2-propyn-1-yl]oxy}-1-azabicyclo[2.2.1]heptan-3-imine | C16H18N2O2 | ChemSpider3Z,4S)-N-{[3-(3-Methoxyphenyl)-2-propyn-1-yl]oxy}-1-azabicyclo[2.2.1]heptan-3-imine | C16H18N2O2 | ChemSpider
Drugs or Compounds in Development. Imaging Agents. Information Aggregators. Journal Publishers via MeSH. ... 1-Azabicyclo[2.2.1]. heptan-3-one, O-[3-. (3-methoxyphenyl)-2. -propyn-1-yl]oxime,. (3Z,4S)- [ACD/Index Name] ...
http://www.chemspider.com/Chemical-Structure.7976092.html
Additional Hetero Ring Which Is Unsaturated Patents and Patent Applications (Class 544/310) - Justia Patents SearchAdditional Hetero Ring Which Is Unsaturated Patents and Patent Applications (Class 544/310) - Justia Patents Search
Abstract: It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell ... Justia Patents Organic Compounds -- Part Of The Class 532-570 Series Patents Organic Compounds (class 532, Subclass 1) ... Abstract: Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): ... Abstract: A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and ...
https://patents.justia.com/patents-by-us-classification/544/310
SDBS-26370
Compound Name. 3-benzoyl-6-oxa-3-azabicyclo(3.1.0)hexane. Molecular Formula. C11H11NO2. ... However we request visitors to our database not to download more than 50 spectra and/or compound information in one day. All ...
https://sdbs.db.aist.go.jp/sdbs/cgi-bin/landingpage?sdbsno=26370
WO1997032857 KAPPA AGONIST COMPOUNDS AND PHARMACEUTICAL FORMULATIONS THEREOFWO1997032857 KAPPA AGONIST COMPOUNDS AND PHARMACEUTICAL FORMULATIONS THEREOF
The compounds of formulae (I), (II), (III) and (IV) have the structure wherein X, X,sub,4,/sub,, X,sub,5,/sub,, X,sub,7,/sub,, ... Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are ... Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, ... HETEROCYCLIC COMPOUNDS. 401. Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring ...
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO1997032857
Talampicillin | Harvard Catalyst Profiles | Harvard CatalystTalampicillin | Harvard Catalyst Profiles | Harvard Catalyst
Bicyclo Compounds [D04.075.080]. *Bicyclo Compounds, Heterocyclic [D04.075.080.875]. *Azabicyclo Compounds [D04.075.080.875.099 ...
https://connects.catalyst.harvard.edu/Profiles/display/Concept/Talampicillin
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
Related compounds cyclize to MACROLIDES. HN - 2008(2004) BX - Acetogenin Compounds MH - Azabicyclo Compounds UI - D053961 MN - ... HN - 2008 MH - Compound Eye, Arthropod UI - D054910 MN - A13.246 MS - Light sensory organ in ARTHROPODS consisting of a large ... The emission of a given device is determined by the active compound used (e.g., gallium arsenide crystals doped with aluminum ... AN - do not confuse with HEART SOUNDS, a physiologic concept HN - 2008 MH - Iron Carbonyl Compounds UI - D054354 MN - D01.485. ...
https://decs.bvs.br/I/dcsnew2008.txt
HeteroCyclesHeteroCycles
This method was applied to the preparation of optically active azabicyclo compounds, which were converted to chiral azabicyclo- ... To more easily synthesize a diverse range of diazido compounds, a facile method for synthesizing diazido compounds bearing a ... 3-Azido-5-(azidomethyl)benzene derivatives are useful compounds for preparing diverse bistriazole compounds and photoaffinity ... β-Trichloroacetylation of Cyclic Amines: Application to Synthesis of Chiral Azabicyclo-N-oxyls. Masami Kuriyama, Satoshi ...
https://heterocycles.jp/newlibrary/libraries/journal/99/2
7-Azabicyclo[2.2.1]heptane as a structural motif to block mutagenicity of nitrosamines<...
Thus, the 7-azabicyclo[2.2.1]heptane structural motif may be useful for the design of nongenotoxic nitrosamine compounds with ... Thus, the 7-azabicyclo[2.2.1]heptane structural motif may be useful for the design of nongenotoxic nitrosamine compounds with ... Thus, the 7-azabicyclo[2.2.1]heptane structural motif may be useful for the design of nongenotoxic nitrosamine compounds with ... Thus, the 7-azabicyclo[2.2.1]heptane structural motif may be useful for the design of nongenotoxic nitrosamine compounds with ...
https://keio.pure.elsevier.com/ja/publications/7-azabicyclo221heptane-as-a-structural-motif-to-block-mutagenicit
DeCSDeCS
Azabicyclo Compounds - Preferred Concept UI. M0499252. Scope note. Bicyclic bridged compounds that contain a nitrogen which has ... Azabicyclo(1.1.0)Butanes. Azabicyclo(2.2.2)Octanes. Azabicyclo(3.3.1)Nonanes. Azabicyclo(4.3.0)Nonanes. Azabicyclo(5.2.2) ... Bicyclic bridged compounds that contain a nitrogen which has three bonds. The nomenclature indicates the number of atoms in ...
https://decs.bvsalud.org/en/ths/resource/?id=52638
Code System Concept
Azabicyclo compound (substance). Code System Preferred Concept Name. Azabicyclo compound (substance). Concept Status. Published ...
https://phinvads.cdc.gov/vads/ViewCodeSystemConcept.action?oid=2.16.840.1.113883.6.96&code=441193001
3-nitrobenzyl 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate - C14H12N2O5, density, melting point, boiling point, structural...3-nitrobenzyl 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate - C14H12N2O5, density, melting point, boiling point, structural...
3-nitrobenzyl 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate - C14H12N2O5, synthesis, structure, density, melting point, ... Nitro Compounds. See other substances:. *2,2,3-trimethyl-3-sulfanylbutanenitrile *tert-butyl 2,2,3-trimethyl-3- ... boiling point of 3-nitrobenzyl 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate , density of 3-nitrobenzyl 7-oxo-1-azabicyclo[ ... 7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (3-nitrophenyl)-methyl ester ...
https://www.chemsynthesis.com/base/chemical-structure-5283.html
Tadalafil Tablets/Oral Jelly Manufacturer & Exporter In IndiaTadalafil Tablets/Oral Jelly Manufacturer & Exporter In India
Aromatic heterocyclic compound *Azabicyclo *Benzenoid *Benzodioxole *Beta-carboline *Carbonyl group *Carboxamide group ...
https://www.weefselpharma.com/products/tadalafil-manufacturer-in-india/
DeCS Ingl s
D02.145 Aza Compounds .. D02.145.074 Azabicyclo Compounds .. D02.145.074.722 Tropanes .. D02.145.074.722.229 Atropine ... D03.605.084 Bridged Bicyclo Compounds, Heterocyclic .. D03.605.084.500 Azabicyclo Compounds .. D03.605.084.500.722 Tropanes .. ... D03.633 Heterocyclic Compounds, Fused-Ring .. D03.633.100 Heterocyclic Compounds, 2-Ring .. D03.633.100.834 Quinolizines .. ... D01.146 Calcium Compounds .. D01.146.375 Calcium Sulfate .. D01.578 Minerals .. D01.578.215 Calcium Sulfate .. D01.875 Sulfur ...
http://trigramas.bireme.br/cgi-bin/mx/[email protected]?collection=DeCSi&lang=p&minsim=0.30&maxrel=10&text=Morphine%20Sulfate%20
Synthesis and evaluation of racemic [<sup>11</sup>C]NS2456 and its enantiomers as selective serotonin reuptake radiotracers...
The compounds crossed the blood-brain barrier rapidly and accumulated preferentially in regions rich in serotonin uptake sites ... keywords = "8-azabicyclo[3.2.1]oct-2-ene, Chiral resolution, PET, Selective serotonin reuptake inhibitor, [C]NS2456", ... The compounds crossed the blood-brain barrier rapidly and accumulated preferentially in regions rich in serotonin uptake sites ... The compounds crossed the blood-brain barrier rapidly and accumulated preferentially in regions rich in serotonin uptake sites ...
https://jhu.pure.elsevier.com/en/publications/synthesis-and-evaluation-of-racemic-sup11supcns2456-and-its-enant
Cefmenoxime | Profiles RNS
Bicyclo Compounds [D04.075.080]. *Bicyclo Compounds, Heterocyclic [D04.075.080.875]. *Azabicyclo Compounds [D04.075.080.875.099 ...
https://profiles.uchicago.edu/profiles/display/35125
Molinstincts l Chemical Compounds DatabaseMolinstincts l Chemical Compounds Database
... info per compound, a total of 8+ billion sets of data based on quantum chemistry, QSPR, and Artificial Neural Network for your ... 4+ million Chemical Compounds, 2,100+ sets of data & ... 3S)-1-azabicyclo[2.2.2]octan-3-yl acetate. SMILES. CC(=O) ... Other Names of This Compound:. Thermo-Physico-Chemical Property Data Available on This Page (Keywords Basis):. Absolute Entropy ... Multiple sets of information for the compounds with high drug-likeness score are readily accessible. ...
https://search.molinstincts.com/analysis/analysis.ce?0001-nnzs
paichongding | Semantic Scholarpaichongding | Semantic Scholar
Azabicyclo Compounds. Pyridines. Papers overview. Semantic Scholar uses AI to extract papers important to this topic. ...
https://www.semanticscholar.org/topic/paichongding/651158
N-cycloheptylpiperidine-4-carboxamide (429632-06-4) - Chemical Safety, Models, Suppliers, Regulation, and...N-cycloheptylpiperidine-4-carboxamide (429632-06-4) - Chemical Safety, Models, Suppliers, Regulation, and...
Similar Compounds. 2-Azabicyclo[2.2.2]octan-3-one (3306-69-2) 2 alternate names ...
http://chemchart.com/n-cycloheptylpiperidine-4-carboxamide-detail.html
Pesquisa | Biblioteca Virtual em Saúde - BRASILPesquisa | Biblioteca Virtual em Saúde - BRASIL
For translational relevance, compounds were tested against clinically relevant T.b. brucei subspecies. Compounds with activity ... Antiprotozoal Activity of Azabicyclo-Nonanes Linked to Tetrazole or Sulfonamide Cores. Dolensky, Johanna; Hinteregger, Clemens ... compound 18c is one of the most potent nitro-containing agents reported against HAT in vitro. Compound 18g revealed an ... to deprioritise compounds with this activity, they were tested against recombinant TcCYP51. Compounds with biological profiles ...
https://pesquisa.bvsalud.org/brasil/?lang=pt&q=au:Kaiser,+Marcel
Registration Dossier - ECHARegistration Dossier - ECHA
2R-(2α,3Z,5α)]-3-(2-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, compound with tert-butylamine ...
https://chesar.echa.europa.eu/web/guest/registration-dossier/-/registered-dossier/10886/6/4/4
BICILLIN® C-R Description (penicillin G benzathine, penicillin G procaine) | Pfizer Medical Information - USBICILLIN® C-R Description (penicillin G benzathine, penicillin G procaine) | Pfizer Medical Information - US
4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid compound with N,N-dibenzylethylenediamine (2:1), tetrahydrate. It occurs ... Penicillin G procaine, (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid ... compound with 2-(diethylamino)ethyl p-aminobenzoate (1:1) monohydrate, is an equimolar salt of procaine and penicillin G. It ...
https://www.pfizermedicalinformation.com/en-us/bicillin-cr/description
Altropane: Uses, Interactions, Mechanism of Action | DrugBank OnlineAltropane: Uses, Interactions, Mechanism of Action | DrugBank Online
Azabicyclo Compounds. *Iodine Radioisotopes. *Tropanes. Chemical TaxonomyProvided by Classyfire. Description. This compound ... Organohalogen compound / Organoheterocyclic compound / Organoiodide / Organonitrogen compound / Organooxygen compound / ... Tropane is an organonitrogenous [3.2.1] bicyclic organic compound.. Kingdom. Organic compounds. Super Class. Alkaloids and ... Carbonyl compounds / Organic oxides / Organofluorides / Organoiodides / Organopnictogen compounds. ...
https://go.drugbank.com/drugs/DB04947
Clavulanic Acids | Profiles RNS
Bicyclo Compounds [D04.075.080]. *Bicyclo Compounds, Heterocyclic [D04.075.080.875]. *Azabicyclo Compounds [D04.075.080.875.099 ... Acids, salts, and derivatives of clavulanic acid (C8H9O5N). They consist of those beta-lactam compounds that differ from ...
https://profiles.rush.edu/display/3315
CharChem. Heterocyclic compounds (2 rings)CharChem. Heterocyclic compounds (2 rings)
6R)-3-(Acetoxymethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid(IUPAC). ; 5-thia-1-azabicyclo[4.2.0]oct-2-ene ... Organic compound » Heterocyclic compound » Heterocyclic compounds (2 rings) Selected category: Heterocyclic compounds (2 rings) ... 2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid(IUPAC). ; 4-thia-1-azabicyclo[3.2.0]heptane-2- ... Categories: Heterocyclic compounds (2 rings) PubChem CID: 798 , ChemSpider ID: 776 , CHEBI:16881 , CHEMBL15844 , MolPort-001- ...
http://www.easychem.org/en/subst-ref/?cat=104
Browsing QO-Artigos by TitleBrowsing QO-Artigos by Title
Methyl 2-diphenylphosphoryloxy-2-azabicyclo[2.2.1]hept-5-ene-3-exocarboxylate  Sousa, Carlos A.D.; Vale, M. Luísa C.; ... In the title compound, C20H20NO4P, the dihedral angle between the phenyl rings is 68.52 (7) . In the crystal structure, the ... Pyrans are privileged heterocyclic structures found in numerous natural compounds with extraordinary biological activities. The ...
https://minerva.usc.es/xmlui/handle/10347/12292/browse?rpp=20&etal=-1&sort_by=1&type=title&starts_with=L&order=ASC
PHA-709829 | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGYPHA-709829 | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY
Compound class. Synthetic organic IUPAC Name N-[(3R,5R)-1-azabicyclo[3.2.1]octan-3-yl]furo[2,3-c]pyridine-5-carboxamide. ... UniChem Compound Search for chemical match using the InChIKey PTGWFYYEAUFEAS-ZYHUDNBSSA-N ...
https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3997
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
Related compounds cyclize to MACROLIDES. HN - 2008(2004) BX - Acetogenin Compounds MH - Azabicyclo Compounds UI - D053961 MN - ... HN - 2008 MH - Compound Eye, Arthropod UI - D054910 MN - A13.246 MS - Light sensory organ in ARTHROPODS consisting of a large ... The emission of a given device is determined by the active compound used (e.g., gallium arsenide crystals doped with aluminum ... AN - do not confuse with HEART SOUNDS, a physiologic concept HN - 2008 MH - Iron Carbonyl Compounds UI - D054354 MN - D01.485. ...
https://decs2014.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
Related compounds cyclize to MACROLIDES. HN - 2008(2004) BX - Acetogenin Compounds MH - Azabicyclo Compounds UI - D053961 MN - ... HN - 2008 MH - Compound Eye, Arthropod UI - D054910 MN - A13.246 MS - Light sensory organ in ARTHROPODS consisting of a large ... The emission of a given device is determined by the active compound used (e.g., gallium arsenide crystals doped with aluminum ... AN - do not confuse with HEART SOUNDS, a physiologic concept HN - 2008 MH - Iron Carbonyl Compounds UI - D054354 MN - D01.485. ...
https://decs2013.bvsalud.org/I/dcsnew2008.txt
NEW (2008) DeCS DESCRIPTORS WITH SCOPE NOTES (UNIT RECORD FORMAT; 21/02/2008
Related compounds cyclize to MACROLIDES. HN - 2008(2004) BX - Acetogenin Compounds MH - Azabicyclo Compounds UI - D053961 MN - ... HN - 2008 MH - Compound Eye, Arthropod UI - D054910 MN - A13.246 MS - Light sensory organ in ARTHROPODS consisting of a large ... The emission of a given device is determined by the active compound used (e.g., gallium arsenide crystals doped with aluminum ... AN - do not confuse with HEART SOUNDS, a physiologic concept HN - 2008 MH - Iron Carbonyl Compounds UI - D054354 MN - D01.485. ...
https://decs2018.bvsalud.org/I/dcsnew2008.txt
BicyclicSynthesisHexaneCephalosporin compoundMedicinalPhenylDopamineThereofBacteriaPreparationsFormulaActiveRapidlyChemicalActivityPropertiesPresentClassSetsSaltGroupHeterocyclicOctaneDerivativesOctan-3-ylMoietyHeptaneOctanesHexanesAtropineMethylSyntheticPotentAntagonistsReceptorDrug CompoundsNitrogenOrganic compoundsSubstancesInorganicIntermediatesPyridinePharmaceuticallyCyclizationSulfur compoundTropaneAqueousElemental analysisAcidReactionsReagentSubstanceDataReactionEsterStabilitySaltsMassFormulaJournal
Bicyclic2
  • Bicyclic bridged compounds that contain a nitrogen which has three bonds. (bvsalud.org)
  • Tropane is an organonitrogenous [3.2.1] bicyclic organic compound. (drugbank.com)
Synthesis2
  • We aim to enable the research community in accelerated discovery via synthesis of complex and difficult to make compounds. (clearsynth.com)
  • A concise synthesis of (±)-karanone, an important aroma compound of agarwood, was achieved from a commercially available 3-methylcyclohex-2-enol in 3.5% yield in 11 steps. (bvsalud.org)
Hexane2
  • 2,6)-Diamino-(5,7)-dihydroxyheptanoic acid (DADH), a non-proteinogenic amino acid, is converted to 1-azabicyclo[3.1.0]hexane ring-containing amino acids that are subsequently incorporated into ficellomycin and vazabitide A. The present study revealed that the sugar aminotransferase-like enzymes Fic25 and Vzb9, with a high amino acid sequence identity (56%) to each other, synthesized stereoisomers of DADH with (6S) and (6R) configurations, respectively. (bvsalud.org)
  • The different stereochemistry at C6 of DADH resulted in a different stereochemistry/orientation of the aziridine portion of the 1-azabicyclo[3.1.0]hexane ring, which plays a crucial role in biological activity, between ficellomycin and vazabitide A. A phylogenic analysis suggested that Fic25 and Vzb9 evolved from sugar aminotransferases to produce unusual building blocks for expanding the structural diversity of secondary metabolites. (bvsalud.org)
Cephalosporin compound3
  • Formulations containing an antibacterial alkali metal salt of a cephalosporin compound and methods of treating or preventing bacterial infections in dogs and cats. (allindianpatents.com)
  • Mannitol, however, was not effective in stabilizing the disclosed cephalosporin compound. (allindianpatents.com)
  • Cefuroxime is a 3-(carbamoyloxymethyl)cephalosporin compound. (macsenlab.com)
Medicinal3
  • Thus, the 7-azabicyclo[2.2.1]heptane structural motif may be useful for the design of nongenotoxic nitrosamine compounds with potential biological/medicinal applications. (elsevier.com)
  • The transfer of nitrogen atoms is extremely valuable in the preparation of medicinal compounds. (researchgate.net)
  • We also offer synthetic support to your medicinal chemistry program by preparing reference compounds, intermediates, and impurities. (chicagodiscoverysolutions.com)
Phenyl1
  • These are compounds containing a phenyl group linked to a tropane moiety. (drugbank.com)
Dopamine1
  • Fenoldopam is a synthetic compound that acts as a selective peripheral dopamine D 1A receptor agonist . (chemeurope.com)
Thereof3
  • Provided herein are compounds of the Formula I: and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, wherein R1, R2, R9, X1 and G are as defined herein, which are inhibitors of one or more TAM kinases and/or c-Met kinase, and are useful in the treatment and prevention of diseases which can be treated with a TAM kinase inhibitor and/or a c-Met kinase inhibitor. (justia.com)
  • The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of one or both of ERK1 and ERK2. (justia.com)
  • Compound I, wherein M is Na+, and the preparation thereof, are disclosed in U.S. Patent Nos. (allindianpatents.com)
Bacteria2
  • Quantitative methods that require measurement of zone diameters provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. (nih.gov)
  • Quantitative methods that are used to determine minimum inhibitory concentrations (MICs) provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. (nih.gov)
Preparations1
  • The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2. (justia.com)
Formula2
  • The invention is also directed to methods for treating bacterial infections in dogs and cats by administering a compound of Formula I. (allindianpatents.com)
  • The compounds of Formula i are broad spectrum cephalosporin antibacterials and are, therefore, useful in the treatment of bacterial infections in animals. (allindianpatents.com)
Active2
  • Compared to the lead compound a diarylthioether was more active and less cytotoxic resulting in an excellent selectivity index of 850. (bvsalud.org)
  • Various potent cocaine analogues and other compounds active at the plasma membrane transporter did not block ligand binding to the vesicular transporter. (nih.gov)
Rapidly2
  • The compounds crossed the blood-brain barrier rapidly and accumulated preferentially in regions rich in serotonin uptake sites (e.g., brainstem, subthalamus and thalamus). (elsevier.com)
  • After addition of diluent, cefamandole nafate rapidly hydrolyzes to cefamandol (cefamandole) e, and both compounds have microbiologic activity in vivo . (rxlist.com)
Chemical2
  • Tetrahedron 56 (2000) 6877-6885, disclose that sucrose improved chemical stability of a befa-lactam compound at a sucrose/drug ratio of 0.1:1 to 0.5:1. (allindianpatents.com)
  • Observed top chemical compounds associated with the concept c_0122 # mined from the 'HETATM' record lines within the wwPDB # coordinate files of this concept's usages. (monash.edu)
Activity2
  • MMV's Malaria Box compound MMV030666 shows multi-stage activity against various strains of Plasmodium falciparum and lacks resistance development. (bvsalud.org)
  • Compounds 2a, 2b, 2e, 2f and 2i further exhibited marginal antifungal activity against Candida parapsilosis. (istanbul.edu.tr)
Properties3
  • Mol-Instincts supplies 35 constant properties of pure organic compounds. (molinstincts.com)
  • Mol-Instincts possesses 11 temperature-dependent properties of pure organic compounds. (molinstincts.com)
  • The structures of the compounds were established by IR, 1 H-NMR, 13C-NMR (APT), electrospray ionization mass spectrometry (ESI-MS) and microanalysis (C, H, N). All of the tested compounds, except for compound 2h, displayed weak antibacterial properties against Staphylococcus epidermidis ATCC 12228 and Staphylococcus aureus ATCC 29213. (istanbul.edu.tr)
Present1
  • The following list identifies those elements which may exist in steel or which may comprise compounds present in steel or alloy steels. (europa.eu)
Class1
  • This compound belongs to the class of organic compounds known as phenyltropanes. (drugbank.com)
Sets1
  • Multiple sets of information for the compounds with high drug-likeness score are readily accessible. (molinstincts.com)
Salt1
  • Penicillin G procaine, (2 S ,5 R ,6 R )-3,3-Dimethyl-7-oxo-6-(2-phenylacetamido)-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid compound with 2-(diethylamino)ethyl p-aminobenzoate (1:1) monohydrate, is an equimolar salt of procaine and penicillin G. It occurs as white crystals or a white, microcrystalline powder and is slightly soluble in water. (pfizermedicalinformation.com)
Group1
  • A straightforward method for the direct introduction of the tert-butoxycarbonyl group into a variety of organic compounds has been developed using flow microreactor systems. (researchgate.net)
Heterocyclic1
  • Study on cyclization reactions of heterocyclic compounds bearing ethynyl and formyl groups in close proximity to each other. (vu.lt)
Octane6
  • In order to discover a medicine effective against Alzheimer's disease, we synthesized a series of quinoline derivatives having a characteristic 1-azabicyclo[3.3.0]octane amine ring, and performed pharmacological evaluation of them. (nih.gov)
  • A series of naphthalene derivatives substituted with the 1-azabicyclo[3.3.0]octane ring were also synthesized and muscarinic M1 and M2 receptor binding affinity determined. (nih.gov)
  • The anxiolytic-like profile of the nociceptin receptor agonist, endo-8-[bis(2-chlorophenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octane-3-carboxamide (SCH 655842): comparison of efficacy and side effects across rodent species. (semanticscholar.org)
  • The 11 C-labelling of a novel tropane derivative (+)-(E)-(1R,2R,3S)-3-(3,4-dichlorophenyl)-8-[ 11 C]methyl-8 -azabicyclo[3.2.1]octane-2-O-methyl-aldoxime (NS 2214 or BMS-204756), an inhibitor of the dopamine transporter (IC 50 3 nM) is reported. (elsevier.com)
  • E)-(1R,2R,3S)-3-(3,4-dichlorophenyl)-8-azabicyclo[3.2.1]octane-2-O-methyl -aldoxime (NS 2262, either as the disulphate salt with added base or as the free amine) was alkylated with [ 11 C]methyl iodide. (elsevier.com)
  • For example, derivatives of a 1-azabicyclo[2.2.2]octane system could have a chiral nitrogen, and the fact that the substituents are tied back prevents inversion of the nitrogen. (stackexchange.com)
Derivatives2
  • These compounds had much higher affinity for M1 receptors than the quinoline derivatives, and 1-[N-(1-azabicyclo[3.3.0]octan-5-yl)methyl-N-methylamino]-4-nitronaph tha lene showed the highest affinity and selectivity. (nih.gov)
  • Reactions of 4-chloromethyl-1,4-dihydropyridine and 4-(l-chloroethyl)-1,4-dihydropyridine derivatives with enolate ions from 3-dicarbonyl compounds have been studied, and shown to give the corresponding 4-substituted-4,5-dihydroazepines under mild conditions. (mun.ca)
Octan-3-yl2
  • The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists. (ox.ac.uk)
  • The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. (ox.ac.uk)
Moiety3
  • They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid. (lookformedical.com)
  • These are compounds containing a 1,2-thiazine fused to a 2-azetidinone to for a oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid moiety or a derivative thereof. (drugbank.com)
  • Furthermore, the structure-activity relationship reveals that within this class of compounds, the diphenylmethyl moiety is constant at the 2-substituent, whereas the 3-substituent is directly correlated with the antagonist activity of the compound. (elsevier.com)
Heptane1
  • Radioligand binding affinities of four new muscarinic antagonists and six potential muscarinic agonists which possess the 2-alkyl-2-azabicyclo[2.2.1]heptane ring system have been determined in rat heart, rat brain, and m1- or m3-transfected CHO cell membrane preparations to examine the selectivity for subtypes of muscarinic receptor. (rti.org)
Octanes1
  • Several classes of compounds, particularly the 2,3-disubstituted azabicyclo-octanes, appear to be relatively potent antagonists at the human MRG-X1 receptors, as confirmed by the receptor trafficking assay and radioligand binding studies. (elsevier.com)
Hexanes2
  • With this approach, a range of spirobarbiturate-3-azabicyclo[3.1.0]hexanes and spirobarbiturate-cyclopropa[ a ]pyrrolizines were obtained in moderate to good yields with excellent diastereoselectivities. (thieme-connect.de)
  • This chapter also provides an overview of published synthetic routes towards ficellomycin and l-azabicyclo[3.1.0]hexanes. (bl.uk)
Atropine2
  • Benztropine mesylate is a synthetic compound containing structural features found in atropine and diphenhydramine. (nih.gov)
  • Aminoalcohol esters a) Solanaceous alkaloids and synthetic analogues: Atropine, Hyoscine b) Synthetic compounds: Propantheline 2. (slideshare.net)
Methyl4
  • Methyl 5-acetyl-2,6-dimethylnicotinate and its dihydro-compound were synthesized, particularly for mass spectral correlations. (mun.ca)
  • The most active compounds, however, were those containing chloro, methyl, or thiomethyl ortho substituents (-), and, in particular, 4-pyridyl analog reinforced the concept that log could be reduced in select cases with only a slight decrease in uptake efficiency. (abt-263.com)
  • Consistent with isoquinuclidine and ABH compounds, des-methyl ABX had the most favorable result in this regard but also the largest drop-off in glycine uptake inhibition. (abt-263.com)
  • The most potent of the analogs was (1R-2-exo-3-exo)-2-(carbomethoxy)-8-methyl-8-azabicyclo (3.2.1) octyl 3-{dollar}\beta{dollar}-styrene. (umaryland.edu)
Synthetic3
  • Antimalarial drugs have thus far been chiefly derived from two sources-natural products and synthetic drug-like compounds. (nih.gov)
  • Here we investigate whether antimalarial agents with novel mechanisms of action could be discovered using a diverse collection of synthetic compounds that have three-dimensional features reminiscent of natural products and are underrepresented in typical screening collections. (nih.gov)
  • Chapter Two describes our synthetic efforts to the l-azabicyclo[3.1.0]hexane core of ficellomycin. (bl.uk)
Potent4
  • The 2,2-diphenylpropionate 5-endo substituted compound was the most potent, showing affinities between 4.23 x 10(-10) and 1.18 x 10(-9) M in rat heart, rat brain, and m1- or m3-transfected CHO cell membrane preparations. (rti.org)
  • One of the less potent compounds was found to inhibit ({dollar}\sp3{dollar}H) cocaine binding and ({dollar}\sp3{dollar}H) dopamine uptake by a mechanism apparently different from that of the nine other analogs. (umaryland.edu)
  • Herein we report the discovery of compound 15 (PF-06795071), a potent and selective covalent MAGL inhibitor, featuring a novel trifluoromethyl glycol leaving group that confers significant physicochemical property improvements as compared with earlier inhibitor series with more lipophilic leaving groups. (inrae.fr)
  • FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively[1].FGI-106 is a potent compound for COVID-19 treament. (dcchemicals.com)
Antagonists3
  • One VMG program is the rodent Hershberger bioassay, which is intended to be used as a screen for suspected androgen agonists and antagonists, and to assist in compound prioritization for further evaluation. (nih.gov)
  • Compounds 47 and 48 were found to be high affinity, selective vasopressin V(1A) antagonists. (ox.ac.uk)
  • Toward this end, we developed a cell-based beta-lactamase (BLA) reporter gene assay to identify small molecule antagonists of the human MRG-X1 receptor from a library of compounds. (elsevier.com)
Receptor4
  • Tests for central nervous muscarinic cholinergic receptor binding affinity indicated that these compounds had higher affinities to muscarinic M1 receptors than to M2 receptors. (nih.gov)
  • A model is presented relating the decreased conformational flexibility, decreased aqueous solvation and increased pK{dollar}\sb{lcub}\rm a{rcub}{dollar}s of the WIN compounds to their increased binding affinity to the cocaine receptor. (umaryland.edu)
  • The present results suggest that both the protonated form and the neutral form of the compounds may bind with high affinity to the cocaine receptor. (umaryland.edu)
  • A cell-based receptor trafficking assay was used to further validate the mechanism of action of these compounds. (elsevier.com)
Drug Compounds1
  • Channelomic studies screen potential drugs for their effectiveness at channelopathies, by examining the binding affinities of candidate drug compounds, by a variety of techniques, including patch clamp electrophysiology, PCR, and immunohistochemistry. (hitachinakaten.com)
Nitrogen3
  • Bicyclic bridged compounds that contain a nitrogen which has three bonds. (uams.edu)
  • HN - 2008(2004) BX - Acetogenin Compounds MH - Acridones UI - D054831 MN - D3.132.32 MN - D3.494.46.109 MS - Compounds based on acridone, which have three linear rings, with the center ring containing a ring nitrogen and a keto oxygen opposite to each other. (nih.gov)
  • The calculations predict the pK{dollar}\sb{lcub}\rm a{rcub}{dollar}s of the tropane nitrogen of the WIN compounds to be higher than in cocaine. (umaryland.edu)
Organic compounds2
  • Hairui Chemical is an excellent manufacturer of organic compounds. (chemindustry.com)
  • This compound belongs to the class of organic compounds known as cephalosporins. (drugbank.com)
Substances1
  • Nitric acid actively oxidizes non-metals metals inorganic compounds and organic substances. (kerone.in)
Inorganic1
  • Inorganic compounds that contain uranium as an integral part of the molecule. (lookformedical.com)
Intermediates1
  • We wish to state that anyone interested in sourcing any special molecules, APIs, Intermediates, Chiral Compounds etc. and feels it is difficult for early completion of tasks, please call on us and TEST US TO GET THE BEST OF US. (manusaktteva.com)
Pyridine1
  • vs ) for pyridine matched pairs, and all compounds contained a low to moderate efflux liability. (abt-263.com)
Pharmaceutically2
  • 3. A method of treatment or prophylaxis of osteoarthritis according to claim 1, wherein the compound of Formula (I), a stereoisomer or a pharmaceutically acceptable salt thereof, is administered orally. (freepatentsonline.com)
  • 5. A method of treatment or prophylaxis of osteoarthritis according to claim 1, wherein the therapeutically effective amount comprises at least one dose of a compound of Formula (I), a stereoisomer or a pharmaceutically acceptable salt thereof, in the range of 0.00001 to 0.1 mg/kg of body weight per day. (freepatentsonline.com)
Cyclization1
  • The pentacyclic alkaloid (±)-meloscine was prepared in 19 steps through a reaction sequence that features a putative azatrimethylenemethane intermediate, generated through cascade cyclization of an allenyl azide substrate, to deliver the core azabicyclo[3.3.0]octadiene substructure. (elsevier.com)
Sulfur compound1
  • I think the Ampicillin I am taking does have a sulfur compound to it. (thelupussite.com)
Tropane1
  • In this series of compounds, the length of the spacer between the aryl group and the tropane skeleton ranged from 1 to 4 bond distances, and conformational flexibility of the linkage and orientation of the aryl ring system were controlled by various types of linkage. (umaryland.edu)
Aqueous1
  • Gas chromatographic-mass spectrometric method for the identification and determination of organotin compounds in aqueous solutions has been employed. (vu.lt)
Elemental analysis1
  • Final compounds have been characterized by their elemental analysis, IR, NMR and mass spectra. (alljournals.cn)
Acid1
  • Compounds 1a-1l in turn were prepared by chlorosulfonation of o-methoxy benzoic acid followed by condensation with 6-fluoro-7-(substituted anilino)-2-aminobenzothiazoles. (alljournals.cn)
Reactions2
  • The reactions of some simpler nucleophiles with these chloro-compounds were also investigated. (mun.ca)
  • Reducing agents and oxidizing agents are chemical compounds involved in redox reactions. (kerone.in)
Reagent1
  • Prior to the analysis organotin compounds were derivatized using sodium tetraethylborate as derivatization reagent. (vu.lt)
Substance1
  • The oxidant is a chemical compound which easily transfers atoms of oxygen or another substance in order to gain an electron. (kerone.in)
Data1
  • The complete list of compounds with pharmacokinetic data, Chemical Abstracts Services numbers, full references, and comments by the authors of this manuscript are available as an Excel file. (aspetjournals.org)
Reaction2
  • An oxidizing agent is a compound or element that is present in a redox (oxidation-reduction) reaction which receives electrons originating from a different species. (kerone.in)
  • Pharmacological evaluation of these candidates by activity-based protein profiling identified 14 as a lead compound, which was then radiolabeled with fluorine-18 via a facile S(N)Ar reaction to form 2-[(18)F]fluoropyridine scaffold. (inrae.fr)
Ester1
  • Cocaine is calculated to be more favorably solvated than the WIN compounds due to the presence of the ester groups in the 2{dollar}\beta{dollar} and 3{dollar}\beta{dollar} moieties. (umaryland.edu)
Stability1
  • Impact of contact with an oxidizing agent with a flammable compound depends on the stability of the oxidizing compounds itself. (kerone.in)
Salts1
  • where the asterisk* indicates the point of attachment to the compound of formula (I) including their agrochemically active salts, metal complexes and N-oxides. (sumobrain.com)
Mass1
  • CoA, MASS, NMR and HPLC will be provided along with the compounds. (vivanls.com)
Formula1
  • 2. A composition characterized by a content of at least one compound of the formula (I) according to claim 1, in addition to auxiliaries. (sumobrain.com)
Journal1
  • Journal of Labelled Compounds and Radiopharmaceuticals , 39 (12), 959-972. (elsevier.com)