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Synthesis and in vitro antimycobacterial activity of 2-methoxybenzanilides and their thioxo analogues

Ján Kozic, Eva Novotná, Marie Volková, Jiřina Stolaříková, František Trejtnar, Jarmila Vinšová

. 2012 ; 56 () : 387-395.

Jazyk angličtina Země Francie

Typ dokumentu časopisecké články, práce podpořená grantem

Perzistentní odkaz   https://www.medvik.cz/link/bmc13024342

Grantová podpora
NS10367 MZ0 CEP - Centrální evidence projektů
NT13346 MZ0 CEP - Centrální evidence projektů

A new series of N-(3/4-substituted phenyl) 4/5-chloro-2-methoxybenzamides and their thioxo analogues have been synthesised and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv, as well as the two atypical strains Mycobacterium kansasii and Mycobacterium avium. Five of the most active compounds were evaluated for cytotoxicity and their ability to inhibit mycobacterial isocitrate lyase, which is responsible for latent survival of Mycobacterium. The results showed that benzthioanilides were more active than the corresponding benzanilides. The most active compound, 4-chloro-2-methoxy-N-(3,4-dichlorophenyl)benzothioamide (4e), had a minimal inhibition concentration (MIC) against M. tuberculosis of 2 μmol L(-1), which was better than the activity of the previously published corresponding salicylanilide.

Citace poskytuje Crossref.org

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