Archiv der Pharmazie (Weinheim) 2003-08-01

Antimycobacterial and antifungal isosters of salicylamides.

Karel Waisser, Milan Pesina, Pavel Holý, Milan Pour, Otakar Bures, Jisí Kunes, Vsra Klimesová, Vladimír Buchta, Petra Kubanová, Jarmila Kaustová

Index: Arch. Pharm. (Weinheim) 336(6-7) , 322-35, (2003)

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Abstract

A set of 40 derivatives of 3-hydroxypicolinic acid and 2-sulfanylbenzoic acid, isosteric to salicylanilides was synthesized. The compounds were evaluated for in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium, Candida albicans, Candida tropicalis, Candida krusei, Candida glabrata, Trichosporon beigelii, Aspergillus fumigatus, Absidia corymbifera, Trichophyton mentagrophytes and Microsporum gypseum. Structure-activity relationships of antimycobacterial activity and antifungal activity against T. mentagrophytes and M. gypseum were analyzed by the Free-Wilson method. An increase in antimycobacterial activity was observed only for the sulfanylbenzoic acid derivatives, especially those with the benzyl moiety. The antifungal activity was not significant.