New Aminocarboxamides with Class III Anti-Arrhythmic Activity

Poppe, H.; Schindler, R; Sauer, Wolfgang; Marx, Degenhard; Bartsch, Reni; Каверина, Н. В.; Lichoscherstow, Arkadi M.; Sokolov, S F; Lyskovtsev, V. V.; Середенин, С. Б.; Борисенко, С. А.

doi:10.1002/(sici)1521-4184(19997)332:7<233::aid-ardp233>3.0.co;2-6

Cited by 5 publications

(14 citation statements)

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“…Several active compounds were founded, MICs of 3-(3-trifluoromethylbenzylamin)-pyrazine-2-carboxamide was 12.5 lg/L against M. tuberculosis H37Rv and 25 lg/L against M. kansasii My 235/80, the MIC of 3-amino-N-(2,4-dimethoxybenzyl)pyrazine-2-carboxamide was 6.25 lg/L against M. tuberculosis H37Rv, the MIC of the standard (PZA) was 25.0 lg/L. [3,4] In vitro hepatotoxicity assay was performed for compounds with MIC <12.5 ug/mL. Basic structure-activity relationships will be presented.…”

Section: Antimycobacterial Evaluation Of New Pyrazinamide Analoguesmentioning

confidence: 93%

“…In contrast, 5-chloroindole and other halogen-substituted indole derivatives provoked concentration dependent increases in the affinity of agonists and partial agonists for the 5-HT 3 A receptor e.g. quipazine's affinity for the 5-HT 3 A receptor was 19 AE 3, 11 AE 1 and 6 AE 1 nM in the absence and presence of 5-chloroindole (10 and 30 lM), respectively. DDP 733 0 s affinity was 2.3 AE 0.5 and 1.6 AE 0.05 nM in the absence and presence of 5-chloroindole (30 mM), respectively.…”

Section: Introductionmentioning

confidence: 95%

“…The compounds were characterized and identified using NMR (1D and 2D), IR, MS-(HRSMS, ESI) and UV spectroscopic methods. 3 The analgesic and antiinflammatory activities of the isolated compounds were studied using the Randall-Selitto and formalin pain tests 4,5 . At the dose of 20 mg/kg, Stereostin, Stereospermin (P < 0.0001) and Stereospermiside (P < 0.05) significantly increased the carrageenaninduced pain threshold compared to the distilled water treated animals.…”

Section: Competitive Intelligence and Commercial Viability Analysis -mentioning

confidence: 99%

“…Methods: In the present study we have used radioligand binding assays, fluorescence indicators and patch clamp electrophysiological recording techniques to explore the allosteric modulation of human 5-HT3A stably expressed in HEK293 cells with the aim to identify potent modulators. Results: 5-Chloroindole and other halogen-substituted indole derivatives (concentrations up to 100 lM) did not compete with [ 3 H]-granisetron for the orthosteric site of the 5-HT 3 A receptor or alter the affinity of the competitive antagonist, ondansetron, for the 5-HT 3 A receptor. In contrast, 5-chloroindole and other halogen-substituted indole derivatives provoked concentration dependent increases in the affinity of agonists and partial agonists for the 5-HT 3 A receptor e.g.…”

Section: Introductionmentioning

confidence: 99%

“…Results: 5-Chloroindole and other halogen-substituted indole derivatives (concentrations up to 100 lM) did not compete with [ 3 H]-granisetron for the orthosteric site of the 5-HT 3 A receptor or alter the affinity of the competitive antagonist, ondansetron, for the 5-HT 3 A receptor. In contrast, 5-chloroindole and other halogen-substituted indole derivatives provoked concentration dependent increases in the affinity of agonists and partial agonists for the 5-HT 3 A receptor e.g. quipazine's affinity for the 5-HT 3 A receptor was 19 AE 3, 11 AE 1 and 6 AE 1 nM in the absence and presence of 5-chloroindole (10 and 30 lM), respectively.…”

Section: Introductionmentioning

confidence: 99%

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Drug Discovery and Development

Oaks¹,

Mitchell²,

Pearson³

et al. 2014

Basic Clin Pharma Tox

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Respiratory burst mediates crucial bactericidal mechanism in neutrophils. However, undesirable respiratory burst leads to pathological inflammation and tissue damage. This study investigates the effect and the underlying mechanism of 2-(4-hydroxy-3-prop-2-enyl-phenyl)-4-prop-2-enyl-phenol (honokiol), a lignan extracted from the stem bark of Magnolia officinalis Rehd. et Wils (Magnoliaceae), on N-formyl-Lmethionyl-L-leucyl-L-phenylalanine (fMLP)-induced human neutrophils activation. Signaling pathways regulated by honokiol to oppose fMLP-induced respiratory burst were evaluated by Lyn kinase (a member of Src kinase family) activity in an in vitro kinase assay and by immunoblotting analysis of downstream phosphorylation targets of Lyn. Briefly, honokiol specific inhibited fMLP-induced superoxide anion production and cathespin G release in a concentration-dependent manner (IC 50 = 9.80 AE 0.21; 14.23 AE 1.43 lM respectively). Further, honokiol specific suppressed fMLP-induced Lyn phosphorylation and Lyn kinase activity. Moreover, honokiol attenuated the signaling followed by Lyn kinase, such as Tec translocation from the cytosol to the inner leaflet of the plasma membrane, phosphorylation of AKT, P38, PLCc2, protein kinase C and membrane localization of p47 phox , however, honokiol did not affect fMLP-induced Hck phosphorylation, Fgr kinase activity, and the signaling followed by Hck/Fgr kinases, such as Vav1 and extracellular signal-regulated kinase phosphorylation. Moreover, honokiol, like PP2, attenuated intracellular calcium concentration. However, honokiol neither inhibited NADPH oxidase activity nor increased cyclicAMP levels. Honokiol is not a competitive or allosteric antagonist of fMLP. Additionally, in an in vivo study, honokiol prevents fMLP-induced neutrophil infiltration in mice. Conclusion: honokiol opposes fMLP-mediated neutrophil activation by inhibiting Lyn activation and subsequent interfered with the activation of PLCc2, AKT, p38, protein kinase C, and p47 phox . 4-HYDROXYBENZALDEHYDE ISOLATED FROM GASTRODIA ELATA, ENHANCED SLEEPING BEHAVIORS THROUGH GABAA-ERGIC SYSTEMSChoi J., Han J., Oh E., Hong J., Yun Y., Yoo H., Oh K.Gastrodia elata (GE), one of famous oriental herb medicine, has been used for the treatment of headache, blood pressure and convulsion. Recent studies have been suggested it has sedative and inhibitory effects of platelet aggregation. 4-Hydroxybenzaldehyde (4-HD) is one of the major compounds of GE, which is well known as an inhibitor of GABA-transaminase. This research was investigated to know whether 4-HD enhanced sleeping behaviors through GABA A ergic systems in mice. 4-HD (50, 100, and 200 mg/kg, p.o.) inhibited locomotor activity in mice. 4-HD not only increased total sleep time, but also decreased sleep latency in pentobarbital induced sleeping mice. 4-HD showed synergistic effects with muscimol, suggesting interactions with GABA A ergic drugs. 4-HD increased intracellular chloride in primary cultured hypothalamic granular cells at the dose-dependent manner. The GABA A re...

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Section: Antimycobacterial Evaluation Of New Pyrazinamide Analoguesmentioning

confidence: 93%

Section: Introductionmentioning

confidence: 95%

Section: Competitive Intelligence and Commercial Viability Analysis -mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 3 more Smart Citations

Drug Discovery and Development

Oaks¹,

Mitchell²,

Pearson³

et al. 2014

Basic Clin Pharma Tox

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ChemInform Abstract: New Aminocarboxamides with Class III Anti‐Arrhythmic Activity.

Schindler¹

1999

ChemInform

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carboxylic amidescarboxylic amides (benzene compounds) Q 0490 -081New Aminocarboxamides with Class III Anti-Arrhythmic Activity.-The synthesis of new aminocarboxamides (I) (44 examples) and their efficacy on the action potential duration and the effective refractory period in vitro are described. Anti-arrhythmic and pro-arrhythmic effects are determined in several animal models in comparison with standard drugs. -(SCHINDLER, RUDOLF; ET AL.; Arch.

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Development of analytical methods for hydrochloride salts of cardiocyclide, a new Russian class III antiarrhythmic

et al. 2007

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Cardiocyclide, a new Russian class III antiarrhythmic agent, was developed at the State V. V. Zakusov Science Research Institute Pharmacology, Russian Academy of Medical Sciences. The aims of the present work were to study the physicochemical properties of the hydrochloride salt of this agent (N 1 -(3-diethylaminopropyl)-N 1 -(p-nitrobenzoyl)aminoacetic acid N,N-dicyclohexylamide HCl) and to develop an analytical method for this compound. IR, 1 H NMR, and UV spectra were obtained for cardiocyclide; its solubility was studied; its melting temperature, weight loss on drying and the transparency, color, and pH of its solutions were determined. The purity of material containing compound I was determined by thin-layer chromatography; quantitative cardiocyclide contents were estimated by non-aqueous titration.

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New Aminocarboxamides with Class III Anti-Arrhythmic Activity

Cited by 5 publications

References 8 publications

Drug Discovery and Development

Drug Discovery and Development

ChemInform Abstract: New Aminocarboxamides with Class III Anti‐Arrhythmic Activity.

Development of analytical methods for hydrochloride salts of cardiocyclide, a new Russian class III antiarrhythmic

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