Synthesis and cardiotonic evaluation of R-sulfonyl derivatives of azaheterocycles

• Authors: Alexander I. Grinevich , Serge V. Litvinenko
• Languages of publication: EN

Abstracts

EN

A series of alfa-sulfonyl-2-(-chloro)hetarylacetonitriles was prepared by the interaction of dichlorodiazines and R-sulfonylacetonitriles. Reaction of nucleophilic substitution of chlorine by different N-H-azoles has been studied. The compounds obtained showed 3 types of activity on cardiac papillary muscles: 1. a biphasic activity with increase in cardiac contractility at low concentration and inhibition in high concentration (1, 2, 4, 12-15), 2. a monophasic inhibitory activity (3, 5, 8-10), 3. non-active compounds (6, 7, 11). The preliminary SAR studies indicate the importance of chlorine atom at position 3 in diazine nucleus and of alkyl substituents in benzimidazole moiety for positive inotropic effects.

Keywords

EN

AZAHETEROCYCLE; CARDIOTONIC ACTION

Discipline

• PHARMACOLOGY: PHARMACOLOGY

• Publisher: Institute of Pharmacology, Polish Academy of Sciences
• Journal: Polish Journal of Pharmacology
• Year: 1993
• Volume: 45
• Issue: 1
• Pages: 95-100

Contributors

author

Alexander I. Grinevich

author

Serge V. Litvinenko

• Document Type: article