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Substituted Benzo[b]thiophenes with Antileucotriene Activity


Authors: M. Nič;  M. Havelková;  M. Terinek;  J. Paleček;  J. Svoboda;  A. Jandera 1;  V. Panajotová 1;  M. Kuchař 1
Authors‘ workplace: Ústav organické chemie Vysoké školy chemicko-technologické, Praha 1 Výzkumný ústav pro farmacii a biochemii, Praha
Published in: Čes. slov. Farm., 1999; , 281-286
Category:

Overview

The cyclizing reaction of cinnamic acid (Ia) with thionyl chloride was optimized and a series of3-chloro-6-subst.benzo[b]thiophene-2-carbonyl chlorides Va-Vn was prepared. Chloride Va wastransformed into a series of N-aryl-3-subst. (Cl, OCH3, OH) benzo[b]thiophene-2-carboxamides VII,IX, X. The drugs were subjected to an evaluation of selected antileucotriene activites in vitro and ofthe anti-inflammatory effect in vivo. In agreement with the assumed mechanism, inhibition of theear inflammation is conditioned by the antileucotriene activity, whereas inhibition of the carrageenoedema is not due to this mechanism alone.

Key words:
subst.benzo[b]thiophene-2-carboxamides – synthesis – antiinflammatory effect –antileucotriene activity

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Labels
Pharmacy Clinical pharmacology

Article was published in

Czech and Slovak Pharmacy


1999 Issue 6

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