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Oximes
Amines
Guanidine
A strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant. (From Martindale, the Extra Pharmacopoeia, 30th ed and Merck Index, 12th ed) It is also used in the treatment of myasthenia and as a fluorescent probe in HPLC.
Guanidines
Halogens
Stereoisomerism
Cyclization
Imidazoles
Copper
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Ionic Liquids
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Netropsin
ESR study on the structure-antioxidant activity relationship of tea catechins and their epimers. (1/606)
The purpose of this study is to examine the relationship between the free radical scavenging activities and the chemical structures of tea catechins ((-)-epigallocatechin gallate (EGCG), (-)-epigallocatechin (EGC) and (-)-epicatechin (EC)) and their corresponding epimers ((-)-gallocatechin gallate (GCG), (-)-gallocatechin (GC) and (+)-catechin ((+)-C)). With electron spin resonance (ESR) we investigated their scavenging effects on superoxide anions (O-.2) generated in the irradiated riboflavin system, singlet oxygen(1O2) generated in the photoradiation-hemoporphyrin system, the free radicals generated from 2,2'-azobis(2-amidinopropane)hydrochloride (AAPH) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical. The results showed that the scavenging effects of galloylated catechins (EGCG and GCG) on the four free radicals were stronger than those of nongalloylated catechins (EGC, GC, EC, (+)-C), and the scavenging effects of EGC and GC were stronger than those of EC and (+)-C. Thus, it is suggested that the presence of the gallate group at the 3 position plays the most important role in their free radical-scavenging abilities and an additional insertion of the hydroxyl group at the 5' position in the B ring also contributes to their scavenging activities. Moreover, the corresponding phenoxyl radicals formed after the reaction with O-.2 were trapped by DMPO and the ESR spectra of DMPO/phenoxyl radical adducts were observed (aN=15.6 G and aHbeta=21.5 G). No significant differences were found between the scavenging effects of the catechins and their epimers when their concentrations were high. However, significant differences were observed at relatively low concentrations, and the lower their concentrations, the higher the differences. The scavenging abilities of GCG, GC and (+)-C were stronger than those of their corresponding epimers (EGCG, EGC and EC). The differences between their sterical structures played a more important role in their abilities to scavenge large free radicals, such as the free radicals generated from AAPH and the DPPH radical, than to scavenge small free radicals, such as O-.2 and 1O2, especially in the case with EGCG and GCG with more bulky steric hindrance. (+info)Polyamine biosynthesis inhibitors alter protein-protein interactions involving estrogen receptor in MCF-7 breast cancer cells. (2/606)
We investigated the effects of polyamine biosynthesis inhibition on the estrogenic signaling pathway of MCF-7 breast cancer cells using a protein-protein interaction system. Estrogen receptor (ER) linked to glutathione-S-transferase (GST) was used to examine the effects of two polyamine biosynthesis inhibitors, difluoromethylornithine (DFMO) and CGP 48664. ER was specifically associated with a 45 kDa protein in control cells. In cells treated with estradiol, nine proteins were associated with ER. Cells treated with polyamine biosynthesis inhibitors in the absence of estradiol retained the binding of their ER with a 45 kDa protein and the ER also showed low-affinity interactions with a number of cellular proteins; however, these associations were decreased by the presence of estradiol and the inhibitors. When samples from the estradiol+DFMO treatment group were incubated with spermidine prior to GST-ER pull down assay, an increased association of several proteins with ER was detected. The intensity of the ER-associated 45 kDa protein increased by 10-fold in the presence of 1000 microM spermidine. These results indicate a specific role for spermidine in ER association of proteins. Western blot analysis of samples eluted from GST-ER showed the presence of chicken ovalbumin upstream promoter-transcription factor, an orphan nuclear receptor, and the endogenous full-length ER. These results show that multiple proteins associate with ER and that the binding of some of these proteins is highly sensitive to intracellular polyamine concentrations. Overall, our results indicate the importance of the polyamine pathway in the gene regulatory function of estradiol in breast cancer cells. (+info)When and why a water-soluble antioxidant becomes pro-oxidant during copper-induced low-density lipoprotein oxidation: a study using uric acid. (3/606)
The inclusion of uric acid in the incubation medium during copper-induced low-density lipoprotein (LDL) oxidation exerted either an antioxidant or pro-oxidant effect. The pro-oxidant effect, as mirrored by an enhanced formation of conjugated dienes, lipid peroxides, thiobarbituric acid-reactive substances and increase in negative charge, occurred when uric acid was added late during the inhibitory or lag phase and during the subsequent extensive propagation phase of copper-stimulated LDL oxidation. The pro-oxidant effect of uric acid was specific for copper-induced LDL oxidation and required the presence of copper as either Cu(I) or Cu(II). In addition, it became much more evident when the copper to LDL molar ratio was below a threshold value of approx. 50. In native LDL, the shift between the antioxidant and the pro-oxidant activities was related to the availability of lipid hydroperoxides formed during the early phases of copper-promoted LDL oxidation. The artificial enrichment of isolated LDL with alpha-tocopherol delayed the onset of the pro-oxidant activity of uric acid and also decreased the rate of stimulated lipid peroxidation. However, previous depletion of alpha-tocopherol was not a prerequisite for unmasking the pro-oxidant activity of uric acid, since this became apparent even when alpha-tocopherol was still present in significant amounts (more than 50% of the original values) in LDL. These results suggest, irrespective of the levels of endogenous alpha-tocopherol, that uric acid may enhance LDL oxidation by reducing Cu(II) to Cu(I), thus making more Cu(I) available for subsequent radical decomposition of lipid peroxides and propagation reactions. (+info)Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers. (4/606)
AIMS: This study constituted the first administration of the oral platelet inhibitor, sibrafiban, to humans. The aim was to investigate the pharmacokinetics and pharmacodynamics of Ro 44-3888, the active principle of sibrafiban, after single ascending oral doses of sibrafiban. Particular emphasis was placed on intersubject variability of the pharmacokinetic and pharmacodynamic parameters of Ro 44-3888. METHODS: The study consisted of three parts. Part I was an open ascending-dose study to determine target effect ranges of sibrafiban. Part II, a double-blind, placebo-controlled, parallel-group study, addressed the intersubject variability of pharmacokinetic and pharmacodynamic parameters of the active principle at a sibrafiban dose achieving an intermediate effect. Part III was a double-blind, placebo-controlled, ascending-dose design covering the complete plasma concentration vs pharmacodynamic response curve of sibrafiban. RESULTS: At sibrafiban doses between 5 mg and 12 mg, the pharmacokinetics of free Ro 44-3888 in plasma were linear whereas those of total Ro 44-3888 were non-linear because of the saturable binding to the glycoprotein IIb-IIIa receptor. Saturation of the GP IIb-IIIa receptor was reached at plasma concentrations of 15.9 ng ml-1. At sibrafiban doses up to 2 mg, ADP-induced platelet aggregation was inhibited by 50%, whereas the inhibition of TRAP-induced platelet aggregation was about 20-30%. At the higher doses, ADP-induced platelet aggregation was almost completely inhibited while a clear dose-response could be observed with TRAP-induced inhibition of platelet aggregation at sibrafiban doses of 5 to 12 mg. Ivy bleeding time increased very steeply with dose with a significant prolongation observed at doses of 5 to 7 mg of sibrafiban (5-7 min, >30 min in one case). At a sibrafiban dose of 12 mg, the stopping criterion for dose escalation (prolongation of the Ivy bleeding time >30 min in three out of four subjects per dose group) was reached. The interindividual coefficients of variation of the integrated pharmacokinetic and pharmacodynamic parameters (AUC and AUE) were below 20%, thus lying well within the pre-set level of acceptance. CONCLUSIONS: With a low intersubject variability of its pharmacokinetic and pharmacodynamic parameters, linear pharmacokinetics and pharmacodynamic effects closely related to its plasma concentrations, Ro 44-3888 has good pharmacological prerequisites for a well controllable therapy of secondary prevention of arterial thrombosis in patients with acute coronary syndrome. (+info)Morphological classification of ganglion cells in the central retina of chicks. (5/606)
Classification of retinal ganglion cells (RGCs) in the chick central retina was studied by retrograde labeling of carbocyanine dye (DiI) and intracellular filling with Lucifer Yellow. Ganglion cells were divided into 4 groups, Group Ic/Is, Group IIc/IIs, Group IIIs, Group IVc, according to sizes of somal area and dendritic field and dendritic branching pattern. Group I cells had small somal area and small dendritic field. They were further divided into 2 subgroups by complexity (subgroup Ic) and simplicity (subgroup Is) of the dendritic arborization. Group II cells had medium-sized soma and dendritic field. They were also divided into subgroup IIc and IIs by the same definitions as those of subgroup Ic and Is. Group IIIs had medium-sized soma, large and simple dendritic arborization. Group IVc in which all cells had large soma, showed large and complex dendritic arborization. Cell populations of each group were 51.8% (subgroup Ic), 21.1% (subgroup Is), 6.2% (subgroup IIc), 14.6% (subgroup IIs), 4.2% (Group IIIs), and 2.1% (Group IVc). Subgroup Ic cells, which were very similar to beta-cells in the mammalian central area, represented about a half of the ganglion cell population. Cells in subgroup Is and IIs, which were not reported in the mammalian retina, were found in the chick central retina in relatively high population (35.7%). Morphological features of chick RGCs in the central retina were considered in comparison with those of other vertebrates. (+info)Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. (6/606)
1. The aim of this study was to investigate the effect of N-(3-(aminomethyl)benzyl)acetamidine (1400W), a selective inhibitor of inducible calcium-independent nitric oxide synthase (iNOS), on the functional and histopathological outcomes of experimental transient focal cerebral ischaemia in rats. 2. Transient ischaemia was produced by the occlusion for 2 h of both the left middle cerebral artery and common carotid artery. Treatments with 1400W (20 mg kg(-1)) or vehicle were started 18 h after occlusion of the arteries and consisted in seven subcutaneous injections at 8 h interval. Ischaemic outcomes and NOS activities (constitutive and calcium-independent NOS) were evaluated 3 days after ischaemia. 3. 1400W significantly reduced ischaemic lesion volume by 31%, and attenuated weight loss and neurological dysfunction. 4. 1400W attenuated the calcium-independent NOS activity in the infarct by 36% without affecting the constitutive NOS activity. 5. These findings suggest that iNOS activation contributes to tissue damage and that selective inhibitors of this isoform may be of interest for the treatment of stroke. (+info)Formation of the aldehydic choline glycerophospholipids in human red blood cell membrane peroxidized with an azo initiator. (7/606)
The production of phospholipid hydroperoxide and aldehydic phospholipid was examined in human red blood cell (RBC) membranes after peroxidation with 2,2-azobis(2-amidinopropane)dihydrochloride (AAPH) or xanthine/xanthine oxidase (XO/XOD/Fe3+). Both radical-generation systems caused a profound decrease in the amount of polyunsaturated fatty acid (PUFA) in choline glycerophospholipid (CGP) and induced formation of peroxidized CGP in RBC membranes to different extents. No consistent generation of peroxidized lipids from CGP was evident after peroxidation with XO/XOD/Fe3+, which caused the apparent decomposition of phospholipids and the formation of large amounts of thiobarbituric acid-reactive substance (TBARS). On the other hand, CGP hydroperoxide was formed as a primary product of peroxidation with AAPH. Aldehydic CGP was also detected as a secondary product of hydroperoxide decomposition in AAPH-peroxidized RBC membranes. Aldehydic CGP was preferentially generated from arachidonoyl CGP rather than from linoleoyl CGP in AAPH-peroxidized membranes. AAPH mainly oxidized CGP to hydroperoxide and aldehydic phospholipids. The sum of hydroperoxide and aldehyde of CGP corresponded to the loss of CGP due to peroxidation by AAPH. This result indicates that CGP was mainly converted into these two oxidized phospholipids in AAPH-peroxidized RBC membranes. (+info)Salt-induced hypertension in Dahl salt-resistant and salt-sensitive rats with NOS II inhibition. (8/606)
Although recent evidence suggests that reduced nitric oxide (NO) production may be involved in salt-induced hypertension, the specific NO synthase (NOS) responsible for the conveyance of salt sensitivity remains unknown. To determine the role of inducible NOS (NOS II) in salt-induced hypertension, we treated Dahl salt-resistant (DR) rats with the selective NOS II inhibitor 2-amino-5,6-dihydro-6-methyl-4H-1,3-thiazine (AMT) for 12 days. Tail-cuff systolic blood pressures rose 29 +/- 6 and 42 +/- 8 mmHg in DR rats given 150 and 300 nmol AMT/h, respectively (P < 0.01, 2-way ANOVA) after 7 days of 8% NaCl diet. We observed similar results with two other potent selective NOS II inhibitors, S-ethylisourea (EIT) and N-[3-(aminomethyl)benzyl]acetamidine hydrochloride (1400W). Additionally, AMT effects were independent of alterations in endothelial function as assessed by diameter change of mesenteric arterioles in response to methacholine using videomicroscopy. We, therefore, conclude from these data that NOS II is important in salt-induced hypertension. (+info)
Ligand-Free Copper-Catalyzed Arylation of Amidines
AMIDINES for veterinary use on LIVESTOCK - cattle, sheep, goats, pig, poultry -, DOGS and CATS against external parasites....
Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides - ePrints Soton
DSpace at KOASAS: Phosphoryl azides as versatile new reaction partners in the Cu-catalyzed three-component couplings
Antibacterial action of some aromatic amines, amidines, amidoximes, guanidines and diguanidines | Biochemical Journal
Author: Abou-Elkhair, Reham A. I. / Subject: aldehydes and DNA - PubAg Search Results
Author: Abou-Elkhair, Reham A. I. / Subject: aldehydes - PubAg Search Results
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Low-dimensional formamidinium lead perovskite architectures via controllable solvent intercalation<...
Synthesis, biological evaluation, and docking studies of N-substituted acetamidines as selective inhibitors of inducible nitric...
Ambiphilic Ligands from the 1,4-benzenebis(amidine) Framework : Sussex Research Online
benzyl 3-(aminomethyl)piperidine-1-carboxylate 315717-76-1 Route Of Synthesis Synthetic Routes
N-(3-Methoxyphenyl)-N-(3-chlorophenyl)formamidine
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Reductive cyclisations of amidines involving aminal radicals - Chemical Communications (RSC Publishing)
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Amidine | definition of amidine by Medical dictionary
Lipid Metabolism sub-cluster 78
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Protein arginine deiminase 4 (PAD4): Current understanding and future by Justin E. Jones, Corey P. Causey et al.
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formamidinium lead iodide/methylammonium lead iodide-based perovskite solar cell
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SYNTHESIS OF AMIDOXIMES USING AN EFFICIENT AND RAPID ULTRASOUND METHOD
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N-(2-amino-5-fluorobenzyl)-4-(N-(pyridine-3-acrylyl)aminomethyl)benzamide
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Latitudinal and intracolony ITS-rDNA sequence variation in the symbiotic...
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Diazirine
In these schemes, amidines can be directly converted to diazirines by hypohalite oxidation. This reaction yields a halogenated ... Graham, W. H. (1965-10-01). "The Halogenation of Amidines. I. Synthesis of 3-Halo- and Other Negatively Substituted Diazirines1 ...
GTP cyclohydrolase II
... specifically in cyclic amidines. The systematic name of this enzyme class is GTP 7,8-8,9-dihydrolase (diphosphate-forming). ...
Succinyl-diaminopimelate desuccinylase
3.5.4: Cyclic amidines/. Aminohydrolases. *Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate ...
HDAC4
3.5.4: Cyclic amidines/. Aminohydrolases. *Guanine deaminase. *Adenosine deaminase. *AMP deaminase. *Inosine monophosphate ...
Benzamidine
It is the simplest aryl amidine. The compound is a white solid that is slightly soluble in water. It is usually handled as the ... Aromatic Amidines as Competitive Inhibitors of Trypsin". The Journal of Biochemistry. 69 (5): 893-899. doi:10.1093/ ...
Superbase
These include the phosphazenes, phosphanes, amidines, and guanidines. Other organic compounds that meet the physicochemical or ... Common superbases of this variety feature amidine, guanidine, and phosphazene functional groups. Strong superbases can be ...
Oxazoline
"Amidines Derived from Pt(IV)-Mediated Nitrile−Amino Alcohol Coupling and Their Zn(II)-Catalyzed Conversion into Oxazolines". ... preceding via an intermediate amidine. Limited research has been done into identifying alternative solvents or catalysts for ...
Pyrimidine
Reaction of the former with amidines to give 2-substituted pyrimidines, with urea to give 2-pyrimidinones, and guanidines to ... Pinner, A. (1884). "Ueber die Einwirkung von Acetessigäther auf die Amidine" [On the effect of acetylacetonate ester on ... Pinner, A. (1885). "Ueber die Einwirkung von Acetessigäther auf die Amidine. Pyrimidin" [On the effect of acetylacetonate ester ... who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name "pyrimidin" in 1885 ...
Mitochondrial amidoxime reducing component 1
MOSC1 has been reported to reduce amidoximes to amidines. Genetic variation in MARC1 has been reported to be associated with ...
Pinner triazine synthesis
The Pinner triazine synthesis describes the preparation of 2-hydroxyl-4,6-diaryl-s-triazines by reaction of aryl amidines and ... This reaction may be extended to halogenated aliphatic amidines. This reaction was first reported by Adolf Pinner in 1890 H. ...
Imidine
Amidine Guanidines Pinner, A. (January 1883). "Ueber die Umwandlung der Nitrile in Imide. Verhalten der Blausäure und des ...
7-Methyl-1,5,7-triazabicyclo(4.4.0)dec-5-ene
doi:10.1007/s10765-019-2540-2. Ishikawa, T. (2009). Superbases for Organic Synthesis: Guanidines, Amidines, Phosphazenes and ...
Carboximidate
They can be hydrolyzed to give esters and by an analogous process react with amines (including ammonia) to form amidines. ... Amidines Esters Oxazoline - the corresponding 5-membered heterocycle Roger, Robert; Neilson, Douglas G. (1961). "The Chemistry ...
Oligonucleotide synthesis
Amidine protecting groups for oligonucleotide synthesis". J. Am. Chem. Soc. 108 (8): 2040-2048. doi:10.1021/ja00268a052. Guzaev ...
Dapansutrile
Thus, leading to the formation of thiomidates, imidates and amidines respectively. The nitrile group of OLT1177 is still not ...
Pinner reaction
A Convenient Route to Imidates and Amidine Salts". Journal of Organic Chemistry. 26 (2): 412. doi:10.1021/jo01061a034.. ... With an excess of alcohol to form an orthoester With ammonia or an amine to form an amidine (di-nitriles may form imidines, for ...
Trichloroacetonitrile
A Convenient Route to Imidates and Amidine Salts". The Journal of Organic Chemistry. 26 (2): 412-418. doi:10.1021/jo01061a034. ...
Netropsin
It belongs to the class of pyrrole-amidine antibiotics. Netropsin binds to the minor groove of AT-rich sequences of double ...
1,5-Diazabicyclo(4.3.0)non-5-ene
It is an amidine base used in organic synthesis. A related compound with related functions is 1,8-diazabicyclo[5.4.0]undec-7- ...
Dihidroorotaza - Википедија, слободна енциклопедија
3.5.4: Cyclic amidines/. Aminohidrolaze. *Guanin deaminaza. *Adenozin deaminaza. *AMP deaminaza. *Inozin monofosfat sintaza ...
Phosphazene
They are stronger bases than regular amine or amidine bases. Protonation takes place at a doubly bonded nitrogen atom. Related ... Cyclodiphosphazane Hexachlorophosphazene Polyphosphazene Superbases for Organic Synthesis: Guanidines, Amidines, Phosphazenes ...
Xylamidine
... is an amidine which serves as a serotonin inhibitor. This agent is prepared by alkylation of 3-methoxyphenol (m- ...
Cyanogen azide
Quantum-chemical calculations concerning the spontaneous rearrangement of the adduct into ring-contracted amidines". ...
Peptidylamidoglycolate lyase
This enzyme belongs to the family of lyases, specifically amidine lyases. The systematic name of this enzyme class is ...
3-Dimethylaminoacrolein
The amidine formed with 2-naphthylamine and the dimethyl sulfate adduct can be cyclized with sodium methoxide to give benzo[f] ... Therefore, 3-dimethylaminoacrolein and vinamidines derived therefrom (composed of vinylogous amidines) or vinamidinium salts ( ... "Synthese und Reaktionen vinyloger Amidacetale und Amidine", Angew. Chem. (in German), 77 (5), p. 219, doi:10.1002/ange. ... be easily transformed with nucleophiles such as alkoxides or amines into the corresponding vinylogous amide acetals or amidines ...
Purine imidazole-ring cyclase
This enzyme belongs to the family of lyases, specifically amidine lyases. The systematic name of this enzyme class is DNA-4,6- ...
Imidazolone
4-Imidazolones arise from the condensation of amidines with 1,2-dicarbonyls such as glyoxal. Bellier, Justine; Nokin, Marie- ...
Hagen Pfundner
degree with a dissertation entitled „The Involvement of Cytochrome P450 in the Biotransformation of Amidines; Investigation ...
Β-Butyrolactone
C.G. Jaffredo; J.-F. Carpentier; S.M. Guillaume (2012). "Controlled ROP of β-butyrolactone simply mediated by amidine, ...
Uldazepam
Thio thionamide is even more prone to amidine formation than the lactam itself. Reaction of thionamide (2) with O-allyl- ...
Amidines | CTD
Amidine Sulfonamides and Benzene Sulfonamides: Synthesis and Their Biological Evaluation
Reductive cyclisations of amidines involving aminal radicals - Chemical Communications (RSC Publishing)
Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ... Reductive cyclisations of amidines involving aminal radicals H. Huang, R. W. Adams and D. J. Procter, Chem. Commun., 2018, 54, ... Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ...
Ligand-Free Copper-Catalyzed Arylation of Amidines
Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ... DMF was the superior solvent for the N-arylation of benzamidines, while MeCN was used in the formation of N-aryl amidines in ... Ligand-Free Copper-Catalyzed Arylation of Amidines. Michelle Cortes-Salva, Corey Garvin and Jon C. Antilla*. *Department of ...
Oxalic Amidines - Protonation Studies and Activity in Lactide Polymerisation - dos Santos Vieira - 2012 - European Journal of...
Experimental Chemotherapy for Chagas Disease: A Morphological, Biochemical, and Proteomic Overview of Potential Trypanosoma...
C. F. Silva, M. B. Meuser, E. M. De Souza et al., "Cellular effects of reversed amidines on Trypanosoma cruzi," Antimicrobial ... E. M. De Souza, P. B. da Silva, A. S. Nefertiti et al., "Trypanocidal activity and selectivity in vitro of aromatic amidine ... A. Daliry, M. Munde, M. Q. Pires et al., "The trypanocidal activity of amidine compounds does not correlated with their binding ... previously known as reversed amidines, have extraordinary activity against both Leishmania [71-73] and T. cruzi [52, 53, 55, 56 ...
Amidine | definition of amidine by Medical dictionary
... amidine explanation free. What is amidine? Meaning of amidine medical term. What does amidine mean? ... Looking for online definition of amidine in the Medical Dictionary? ... Amidine , definition of amidine by Medical dictionary https://medical-dictionary.thefreedictionary.com/amidine ... amidine. Also found in: Dictionary, Encyclopedia, Wikipedia. am·i·dine. (ami-dēn), The monovalent radical -C(NH)-NH2. ...
Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric...
Amidine systems are intermediate in structure between tertiary amines and quaternary compounds, at least as regards ionization ... Amidines (guanidine, formamidine, and acetamidine) were introduced as substitutes for the cationic heads present in atropine, ... Thus, amidine moieties are effective bioisosteric substitutes for conventional cationic heads present in antimuscarinic agents ... Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. A useful bioisosteric ...
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity...
Antibacterial action of some aromatic amines, amidines, amidoximes, guanidines and diguanidines | Biochemical Journal
Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides - ePrints Soton
Amidines can be synthesised in a one-pot procedure via imidates.. imidate, thioimidate, amidine, palladium homogeneous ... Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides. Palladium-catalysed coupling between ... Keywords: imidate, thioimidate, amidine, palladium homogeneous catalysis multicomponent reactionscarbonylation, derivatives ... Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides. ...
Cl-Amidine (trifluoroacetate salt), CAS 1043444-18-3 | Cayman Chemical | Biomol.com
Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4 in vitro ... Product information "Cl-Amidine (trifluoroacetate salt)" Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s ... Cl-amidine is cytotoxic to HL-60, MCF7, and HT-29 cancer cell lines (IC50s = 0.25, 0.05 and 1 µM, respectively). In a collagen- ... Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s = 0.8, 6.2, and 5.9 µM for... more ...
Synthesis of Thieno[2,3-d]imidazoles by Copper-Catalyzed Amidine Cyclization - Enamine
A new synthetic approach to thieno[2,3-d]imidazoles is presented on the basis of the N′-(3-halothiophen-2-yl)amidine ... Synthesis of Thieno[2,3-d]imidazoles by Copper-Catalyzed Amidine Cyclization. Synlett , 2014, 25 (07), 965-968 ... Synthesis of Thieno[2,3-d]imidazoles by Copper-Catalyzed Amidine Cyclization ...
Amidine - Wikipedia
Examples of amidines include: DBU diminazene benzamidine Pentamidine Paranyline A common route to primary amidines is the ... Dimethylformamide acetal reacts with primary amines to give amidines: Me2NC(H)(OMe)2 + RNH2 → Me2NC(O)NHR + 2 MeOH Amidines are ... Carboxamidines are frequently referred to simply as amidines, as they are the most commonly encountered type of amidine in ... Amidines are organic compounds with the functional group RC(NR)NR2, where the R groups can be the same or different. They are ...
Conflict of interest: use of pyrethroids and amidines against tsetse and ticks in zoonotic sleeping sickness endemic areas of...
The private veterinary market is divided between products only effective against ticks (amidines) and those effective against ... Bardosh, K., Waiswa, C. & Welburn, S.C. Conflict of interest: use of pyrethroids and amidines against tsetse and ticks in ... The sale of acaricide varied by price, dilution rate and availability (see Table 3). Amidine-based products (which were ... Conflict of interest: use of pyrethroids and amidines against tsetse and ticks in zoonotic sleeping sickness endemic areas of ...
Efficient microwave access to polysubstituted amidines from imidoylbenzotriazoles. - Semantic Scholar
... of microwave synthesis and introduce a new application of imidoylbenzotriazoles in the preparation of polysubstituted amidines. ... Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa ... Efficient microwave access to polysubstituted amidines from imidoylbenzotriazoles.. *. Alan R. Katritzky, Chunming Cai, Sandeep ... Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa ...
Faculty Collaboration Database - Mesh term Amidines
Chiral ferrocenyl amidines as modular ligands for applications in asymmetric catalysis - Research Collection
Chiral ferrocenyl amidines as modular ligands for applications in asymmetric catalysis. * Mendeley ... ASYMMETRISCHE KATALYSE (CHEMISCHE REAKTIONEN); AMIDINE (ORGANISCHE CHEMIE); CYCLOPENTADIENYLKOMPLEXE (KOMPLEXCHEMIE); ... ORGANISCHE SYNTHESE (CHEMIE); ASYMMETRIC CATALYSIS (CHEMICAL REACTIONS); AMIDINES (ORGANIC CHEMISTRY); CYCLOPENTADIENYL ...
Reductive cyclisations of amidines involving aminal radicals | Research Explorer | The University of Manchester
Reductive cyclisations of amidines involving aminal radicals. Research output: Contribution to journal › Article ... Amidines bearing simple alkenes undergo aminal radical cyclisation upon treatment with SmI2. The mild, reductive electron ... HomeResearchResearch ExplorerPublicationsReductive cyclisations of amidines involving aminal radicals ...
The Sydney eScholarship Repository: Novel polyamide amidine anthraquinone platinum(II) complexes for enhancing DNA binding and...
Amidines - Miscellaneous Functional Groups - Functional Groups - Building Blocks
Synthesis of cyclic amidines pka - Help Your Studies
Synthesis of cyclic amidines pka. November 23, 2018. MiaArgumentative Essays Das, d. after synthesis of cyclic amidines pka ... amidines pka amidines suitcase size guide liters to cubic inches followed by spontaneous cyclization to yield cyclic amidines, ... synthesis of cyclic amidines pka synthesis of medium-ring bicyclic diamines by the alkylation and cleavage of cyclic amidines. ... is a hereditary neuromuscular disease synthesis of cyclic amidines pka marked by the progressive weakness and muscle loss, with ...
US Patent Application for SOLVENT APPLICATION IN BOTTLE WASH USING AMIDINE BASED FORMULAS Patent Application (Application ...
... adhesives from a plurality of surfaces through the use of an aqueous or non-aqueous basic organic solvent and/or an amidine, ... Amidine Solvents. In an aspect, an amidine solvent is included in the label removing composition. An amidine solvent is a non- ... Amidine Solvents 1-20 5-20 7-15 Additional Solvents 0.01-15 0.1-15 5-15 Surfactants 0-50 5-40 10-30 Water 5-90 10-80 20-70 ... Amidine Solvents 30-70 40-70 50-65 Additional Solvents 5-50 10-50 20-40 Surfactants 5-50 5-25 10-20 Sodium Hydroxide (caustic) ...
"Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine" by Alexander A. Chumanevich, Corey P. Causey et al.
Interestingly, Cl-amidine drives apoptosis of inflammatory cells in vitro and in vivo, providing a mechanism by which Cl- ... In total, these data help validate the PADs as therapeutic targets for the treatment of IBD and further suggest Cl-amidine as a ... Results are consistent with this hypothesis, as demonstrated by the finding that Cl-amidine treatment, both prophylactic and ... Cl-amidine), could suppress colitis in a dextran sulfate sodium mouse model. ...
Amidine functionality as a stimulus-responsive building block
Dabigatran Amidine Impurity Manufacturer, Dabigatran Amidine Impurity Exporter, Supplier
Adamantane-like molecules, Amidines, Bases (chemistry)
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Chemical Safety, Models, Suppliers, Regulation, and Patents
Tetrodotoxin (TTX) is a potent neurotoxin. Its name derives from Tetraodontiformes, an order that includes pufferfish, porcupinefish, ocean sunfish, and triggerfish; several of these species carry the toxin. Although tetrodotoxin was discovered in these fish and found in several other aquatic animals (e.g., in blue-ringed octopuses, rough-skinned newts, and moon snails), it is actually produced by certain infecting or symbiotic bacteria like Pseudoalteromonas, Pseudomonas, and Vibrio as well as other species found in the animals ...
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Table of Contents - May 21, 1943, 97 (2525) | Science
Plus it
This indicates Cl-amidine blunts basal oxidative bursts. One hour after activation with IFN-γ, Cl-amidine-treated cells have 60 ... Cl-Amidine.. The synthesis of Cl-amidine has been described previously (Luo et al., 2006; Causey and Thompson, 2008). ... Cl-Amidine Delivered through the Drinking Suppresses DSS-Induced Colitis.. We previously showed that Cl-amidine, delivered ... Figure 4B shows that Cl-amidine (10 µg/ml) inhibits oxidative bursts in cultured macrophages. Cells pretreated with Cl-amidine ...
SynthesisDerivativesGuanidineAminesGuanidinesCyclic amidinesInhibitorLigandsArylCitrullinationSuppressesCarboxylicVitroInhibitReactionAlkylationInflammatoryMolecularSuppress colitisFormamidineImidateCytotoxicCompoundsCyclizationEfficacyHypothesisDihydrochlorideInhibitionGroup is replacedCompoundMiceTherapeuticInflammationActive ingredientsCHEMISTRYAtomsBasesMicrowave
Synthesis10
- Gupta, Synthesis and anti-inflammatory activity evaluation of some sulfonamide and amidine derivatives of 4-aryl-3-(2 or 4-picolyl)-2-imino- 4-thiazolines, Indian J. (thefreedictionary.com)
- Synthesis and biological evaluation of new antimuscarinic compounds with amidine basic centers. (nih.gov)
- Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. (nih.gov)
- Saluste, C. Gustaf , Whitby, Richard J. and Furber, Mark (2001) Palladium-catalysed synthesis of imidates, thioimidates and amidines from aryl halides. (soton.ac.uk)
- Das, d. after synthesis of cyclic amidines pka esterification of the carboxyl function, the bromine atoms are nucleophilically substituted and the corresponding diamino compound is obtained. (masterdam.info)
- t1 - synthesis of cyclic amidines pka synthesis of medium-ring bicyclic diamines by the alkylation and cleavage of cyclic amidines. (masterdam.info)
- selective synthesis of aminoisoquinolines via rh(iii)-catalyzed gawharet el fan darbuka review journal newspaper c-h/n-h bond functionalization of heap sort worst case scenario book n-aryl amidines with cyclic kesalahan tata bahasa upsr english paper 2-diazo-1,3-diketones. (masterdam.info)
- acyclic and cyclic acetals of various carbonyl compounds were obtained in excellent yields in factory pollution essay for spm the presence of trialkyl orthoformate and a catalytic amount synthesis of cyclic amidines pka of tetrabutylammonium tribromide in absolute alcohol read "palladium‐catalyzed synthesis of cyclic amidines and imidates. (masterdam.info)
- cheminform" on deepdyve, the largest online rental service thesis statement examples definition essay for scholarly research with thousands of academic publications available at your fingertips read "microwave‐enhanced synthesis of cyclic amidines. (masterdam.info)
- A fast and convenient synthesis of aryl amidines starting from carboxylic acids and cyanamides is reported. (mendeley.com)
Derivatives7
- Derivatives of oxoacids RnE(=O)OH in which the hydroxy group is replaced by an amino group and the oxo group is replaced by =NR. Amidines include carboxamidines, sulfinamidines and phosphinamidines. (mdibl.org)
- It has been known for some time that amidine and guanidine derivatives will inhibit C-mediated hemolysis (i.e. (thefreedictionary.com)
- Amidines (guanidine, formamidine, and acetamidine) were introduced as substitutes for the cationic heads present in atropine, scopolamine, and corresponding quaternary derivatives. (nih.gov)
- The new amidine derivatives proved effective as spasmolytic agents, with little tendency to cause central effects. (nih.gov)
- Topological-mathematical models based on multiple linear regression analyses have been built to predict the reaction yields and the anti-inflammatory activity of a set of heterocylic amidine derivatives, synthesized under environmental friendly conditions, using microwave irradiation. (mdpi.com)
- These models also enabled the screening of virtual libraries for new amidine derivatives predicted to show higher values of reaction yields and anti-inflammatory activity. (mdpi.com)
- Pla-Franco J, Gálvez-Llompart M, Gálvez J, García-Domenech R. Application of Molecular Topology for the Prediction of Reaction Yields and Anti-Inflammatory Activity of Heterocyclic Amidine Derivatives. (mdpi.com)
Guanidine2
- This mini-review describes basic features and applications of small molecules and macromolecules containing amidine, and to a lesser extent, guanidine functional groups. (edu.au)
- Three PFPA homopolymers of different molecular weights were reacted with the commercially available amidine and guanidine species histamine (HIS) dihydrochloride and L-arginine methyl ester (ARG) dihydrochloride in the presence of S-methyl methanethiosulfonate to yield, quantitatively, the corresponding amidine and guanidine-based acrylamido homopolymers. (edu.au)
Amines4
- Amidine systems are intermediate in structure between tertiary amines and quaternary compounds, at least as regards ionization and electronic properties, but differ from the latter in shape (planar not tetrahedral). (nih.gov)
- Dimethylformamide acetal reacts with primary amines to give amidines: Me2NC(H)(OMe)2 + RNH2 → Me2NC(O)NHR + 2 MeOH Amidines are much more basic than amides and are among the strongest uncharged/unionized bases. (wikipedia.org)
- Microwave reactions of primary and secondary amines with imidoylbenzotriazoles 6a-w gave diversely substituted amidines 7a-Aa in 76-94% yields. (semanticscholar.org)
- Some of the groups that were employed for this purpose were amines, amidines, guanidines, and quaternary ammonium. (opioids.com)
Guanidines1
- 5 Amidines and Guanidines in Medicinal Chemistry. (wikipedia.org)
Cyclic amidines1
- This enzyme belongs to the family of hydrolases , those acting on carbon-nitrogen bonds other than peptide bonds, specifically in cyclic amidines. (wikipedia.org)
Inhibitor11
- Cl-amidine is an inhibitor of protein arginine deiminases (PAD, IC50s = 0.8, 6.2, and 5.9 µM for. (biomol.com)
- Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (umassmed.edu)
- Because PAD levels are elevated in mouse and human colitis, we hypothesized that a novel small-molecule inhibitor of the PADs, i.e., chloramidine (Cl-amidine), could suppress colitis in a dextran sulfate sodium mouse model. (umassmed.edu)
- and Hofseth, Lorne J., "Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. (umassmed.edu)
- We previously showed that Cl-amidine, a small-molecule inhibitor of the protein arginine deiminases, suppresses colitis in mice. (aspetjournals.org)
- Structure of the pan-PAD inhibitor, Cl-amidine. (aspetjournals.org)
- Given these findings, we evaluated whether N-α-benzoyl-N5-(2-chloro-1-iminoethyl)- l -ornithine amide (Cl-amidine), a recently described pan-PAD inhibitor, could affect the development of arthritis and autoimmunity by treating mice in the CIA model with Cl-amidine on days 0-35. (jimmunol.org)
- The efficacy of the PADI inhibitor, Cl-amidine, was tested in vitro using MCF10DCIS cells grown in 2D-monolayers and 3D-spheroids, and in vivo using MCF10DCIS tumor xenografts. (biomedcentral.com)
- Next, we show that a PADI inhibitor, Cl-amidine, strongly suppresses the growth of MCF10DCIS monolayers and tumor spheroids in culture. (biomedcentral.com)
- Lastly, we performed cell cycle array analysis of Cl-amidine treated and control MCF10DCIS cells, and found that the PADI inhibitor strongly affects the expression of several cell cycle genes implicated in tumor progression, including p21 , GADD45α , and Ki67 . (biomedcentral.com)
- Interestingly, treatment of several PADI4-expressing cancer cell lines with the PADI inhibitor, Cl-amidine, elicited strong cytotoxic effects while having no observable effect on non-cancerous lines [ 11 ], suggesting that PADIs may represent targets for new cancer therapies. (biomedcentral.com)
Ligands1
- Due to interest in the coordination chemistry of formamidines, the non-symmetric amidine ligands PhNC(Me)NHPri, PhNC(Et)NHPri, and (2,4,6-Me3C6H2)NC(Me)NHPri, have been synthesized, and their reaction with Os3(CO)10(MeCN)2 has been investigated. (unt.edu)
Aryl4
- Copper-catalyzed cross-coupling reactions of amidine salts with aryl iodides give monoarylated amidines in good yields under ligand-free conditions. (organic-chemistry.org)
- DMF was the superior solvent for the N -arylation of benzamidines, while MeCN was used in the formation of N -aryl amidines in good yield. (organic-chemistry.org)
- The reaction was achieved by palladium(II)-catalysis in a one-step microwave protocol using [Pd(O2 CCF3 )2 ], 6-methyl-2,2'-bipyridyl and trifluoroacetic acid (TFA) in N-methylpyrrolidinone (NMP), providing the corresponding aryl amidines in moderate to excellent yields. (mendeley.com)
- With only two freely rotatable bonds, molecular modeling suggests that one amidine group is positioned into the S1 pocket, forming hydrogen bonds with the side chain of Asp189, similar to other amidine-based inhibitors, with the second benzamidine positioned into the S4 pocket in a position to form strong cation-pi bonding with the S4 aryl cage. (researchwithrutgers.com)
Citrullination4
- Because colitis is defined as inflammation of the colon associated with infiltration of white blood cells that release free radicals and citrullination is an inflammation-dependent process, we asked whether Cl-amidine has antioxidant properties. (aspetjournals.org)
- Cl-amidine treatment reduced total synovial and serum citrullination, decreased clinical disease activity by ∼50%, and significantly decreased IgG2a anti-mouse type II collagen Abs. (jimmunol.org)
- Cl-amidine may represent a novel class of disease-modifying agents that modulate aberrant citrullination, and perhaps other immune processes, necessary for the development of inflammatory arthritis. (jimmunol.org)
- For a mechanistic study of Cl-amidine, we explored the idea that Cl-amidine may be preventing the citrullination and/or hyperactivity of DNA methyltransferases (DNMTs). (sc.edu)
Suppresses1
- Interestingly, Cl-amidine drives apoptosis of inflammatory cells in vitro and in vivo, providing a mechanism by which Cl-amidine suppresses colitis. (umassmed.edu)
Carboxylic1
- When the parent oxoacid is a carboxylic acid, the resulting amidine is a carboxamidine or carboximidamide (IUPAC name). (wikipedia.org)
Vitro2
- Because epithelial cell DNA damage associated with colitis is at least in part a result of an oxidative burst from overactive leukocytes, we tested the hypothesis that Cl-amidine can inhibit leukocyte activation, as well as subsequent target epithelial cell DNA damage in vitro and in vivo. (aspetjournals.org)
- In vitro studies indicated that Cl-amidine may act as a tumor suppressor by upregulating miR-16, a putative tumor suppressor miRNA with cell cycle targets, and causing G1 cell cycle arrest. (sc.edu)
Inhibit2
- Reduced levels of citrullinated synovial proteins observed in mice treated with Cl-amidine are consistent with the notion that Cl-amidine derives its efficacy from its ability to inhibit the deiminating activity of PADs. (jimmunol.org)
- Chlor-amidine (Cl-amidine) is designed to irreversibly inhibit PADs through covalent modification at the active site of the enzymes. (sc.edu)
Reaction1
- Examples of amidines include: DBU diminazene benzamidine Pentamidine Paranyline A common route to primary amidines is the Pinner reaction. (wikipedia.org)
Alkylation2
- Asymmetric α-alkylation of N′-tert-butanesulfinyl amidines. (elsevier.com)
- Fingerprint Dive into the research topics of 'Asymmetric α-alkylation of N′-tert-butanesulfinyl amidines. (elsevier.com)
Inflammatory2
- In a collagen-induced mouse model of inflammatory arthritis, Cl-amidine dose-dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies. (biomol.com)
- Inducible nitric oxide synthase, an inflammatory marker, was also downregulated in macrophages by Cl-amidine. (aspetjournals.org)
Molecular1
- The observed structure-activity relationship for the furan-amidine series with NQO2 was rationalized by preliminary molecular docking and binding mode analysis. (aston.ac.uk)
Suppress colitis1
- Results are consistent with this hypothesis, and because DNA damage is a procancerous mechanism, our data predict that Cl-amidine will not only suppress colitis, but we hypothesize that it may prevent colon cancer associated with colitis. (aspetjournals.org)
Formamidine1
- The simplest amidine is formamidine, HC(=NH)NH2. (wikipedia.org)
Imidate1
- The furan ring has been changed to other heterocycles (imidazole, N-methylimidazole, oxazole, thiophene) and the amidine group has been replaced with imidate, reversed amidine, N-arylamide and amidoxime to probe NQO2 activity, improve solubility and decrease basicity of the lead furan amidine. (aston.ac.uk)
Cytotoxic1
- Cl-amidine is cytotoxic to HL-60, MCF7, and HT-29 cancer cell lines (IC50s = 0.25, 0.05 and 1 µM, respectively). (biomol.com)
Compounds2
- These amidines are electrically neutral in undisturbed water, but when carbon dioxide bubbles through, the compounds transform into amidinium bicarbonate salts that act as surfactants. (thefreedictionary.com)
- Amidines are organic compounds with the functional group RC(NR)NR2, where the R groups can be the same or different. (wikipedia.org)
Cyclization1
- A new synthetic approach to thieno[2,3-d]imidazoles is presented on the basis of the N′-(3-halothiophen-2-yl)amidine cyclization under copper-catalyzed cross-coupling. (enamine.net)
Efficacy1
- Next, we tested the efficacy of Cl-amidine in the HCT116 colon cancer cell line and the Azoxymethane (AOM)/Dextran Sulfate Sodium (DSS) murine model of UC. (sc.edu)
Hypothesis2
- Results are consistent with this hypothesis, as demonstrated by the finding that Cl-amidine treatment, both prophylactic and after the onset of disease, reduced the clinical signs and symptoms of colitis, without any indication of toxic side effects. (umassmed.edu)
- Our results showed that in the AOM/DSS murine model of UC-associated CRC, Cl-amidine significantly inhibited tumorigenesis, further supporting our hypothesis. (sc.edu)
Dihydrochloride1
- The initiator, 2,2'-azobis (2-metilpropion amidine ) dihydrochloride (V50, Aldrich) was used as received. (thefreedictionary.com)
Inhibition2
- The analogues were evaluated for inhibition of NQO2, which showed lower activity than the lead furan amidine. (aston.ac.uk)
- Cl-amidine also reduced the methylation of the miR-16 promoter as effectively as DNMT inhibition. (sc.edu)
Group is replaced1
- The −OH group is replaced by an −NH2 group and the =O group is replaced by =NR, giving amidines the general structure RnE(=NR)NR2. (wikipedia.org)
Compound2
- The cyano compound 4 was converted to amidine according to a standard procedure [7]. (thefreedictionary.com)
- Treatment of the resulting compound with ammonia then completes the conversion to the amidine. (wikipedia.org)
Mice2
- Additionally, histopathology scores and total complement C3 deposition were significantly lower in Cl-amidine-treated mice compared with vehicle controls. (jimmunol.org)
- We then carried out preclinical studies in nude (nu/nu) mice and found that Cl-amidine also suppressed the growth of xenografted MCF10DCIS tumors by more than 3-fold. (biomedcentral.com)
Therapeutic2
- In total, these data help validate the PADs as therapeutic targets for the treatment of IBD and further suggest Cl-amidine as a candidate therapy for this disease. (umassmed.edu)
- At a dosage close to the therapeutic one amidines can show a sedative effect in cattle . (parasitipedia.net)
Inflammation1
- We showed that Cl-amidine effectively reduced inflammation, oxidative stress produced by activated leukocytes, and DNA damage. (sc.edu)
Active ingredients1
- Amidines (also called formamidines) are a special group of active ingredients with activity against ticks , mites and lice . (parasitipedia.net)
CHEMISTRY1
- Carboxamidines are frequently referred to simply as amidines, as they are the most commonly encountered type of amidine in organic chemistry. (wikipedia.org)
Atoms1
- At these pH values, the nucleophilic attack of an R-N[H.sub.2] on one of the two outer backbone carbon atoms of dimethyl pimelimidate produces a tetrahedral intermediate that splits into the amidine link and methanol. (thefreedictionary.com)
Bases1
- Cyclic amidine bases such as DBU also support rapid and efficient BUR cures. (thefreedictionary.com)
Microwave1
- Efficient microwave access to polysubstituted amidines from imidoylbenzotriazoles. (semanticscholar.org)