title: N-benzylsalicylthioamides: highly active potential antituberculotics.
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.
authors.affiliation: Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Hradec Králové, Czech Republic.
authors.forename: Rafael
authors.initials: R
authors.lastname: Dolezal
authors.forename: Karel
authors.initials: K
authors.lastname: Waisser
authors.forename: Eva
authors.initials: E
authors.lastname: Petrlíková
authors.forename: Jirí
authors.initials: J
authors.lastname: Kunes
authors.forename: Lenka
authors.initials: L
authors.lastname: Kubicová
authors.forename: Milos
authors.initials: M
authors.lastname: Machácek
authors.forename: Jarmila
authors.initials: J
authors.lastname: Kaustová
authors.forename: Hans Martin
authors.initials: HM
authors.lastname: Dahse
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival; D004305:Dose-Response Relationship, Drug; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009161:Mycobacterium / Q000187:drug effects*; D009162:Mycobacterium avium / Q000187:drug effects; D019909:Mycobacterium kansasii / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D013329:Structure-Activity Relationship; D013854:Thioamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity
chemical_list: D000995:Antitubercular Agents; D013854:Thioamides