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  • Title: N-benzylsalicylthioamides: highly active potential antituberculotics.
    Author: Dolezal R, Waisser K, Petrlíková E, Kunes J, Kubicová L, Machácek M, Kaustová J, Dahse HM.
    Journal: Arch Pharm (Weinheim); 2009 Feb; 342(2):113-9. PubMed ID: 19137534.
    Abstract:
    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.
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