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N‐ Benzylsalicylthioamides: Highly Active Potential Antituberculotics
Author(s) -
Doležal Rafael,
Waisser Karel,
Petrlíková Eva,
Kuneš Jirí,
Kubicová Lenka,
Machácek Miloš,
Kaustová Jarmila,
Dahse Hans Martin
Publication year - 2009
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200800032
Subject(s) - antimycobacterial , lipophilicity , mycobacterium kansasii , chemistry , mycobacterium tuberculosis , moiety , isoniazid , biological activity , quantitative structure–activity relationship , in vitro , stereochemistry , structure–activity relationship , mycobacterium , biochemistry , tuberculosis , bacteria , biology , medicine , pathology , genetics
A gseries of 29 new derivatives of N ‐benzylsalicylthioamides was synthesized and the compounds were tested for in‐vitro antimycobacterial activity against Mycobacterium tuberculosis , Mycobacterium kansasii , and Mycobacterium avium . The activity was analyzed by quantitative structure‐activity relationship (QSAR). Activity increased with increasing lipophilicity and electron donating effect of the substituents in the acyl moiety and decreased with the electrophilic superdelocalizability of the molecules. The most active compounds are more active than isoniazid (INH) and are active against INH‐resistant potential pathogenic strains of mycobacterium.