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Synthesis and cardiotonic evaluation of R-sulfonyl derivatives of azaheterocycles

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Grinevich A. I., Litvinenko S. V.
Polish Journal of Pharmacology
|
1993
|
vol. 45
|
issue 1
95-100
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.
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