[Relation between chemical structure, antitubercular activity and hepatotoxicity of 2-alkylthio-6-benzamidobenzothiazoles].
The paper investigates the relationships between hydrophobic parameters and antituberculotic activity of 2-alkylthio-6-benzamidobenzothiazoles, tested on INH-resistant strain of Mycobacterium tuberculosis. In the group of compounds with linear alkyl substituents in position 2, the tuberculostatic effect is increasing with decrease of lipophility of alkyls. Branching of the alkyls strongly increases the activity. The hepatotoxicity of compounds under study was investigated by means of the activity of serum aminotransferases (ALT, AST) in Wistar type rats. The hepatotoxicity of compounds seemed to be smaller than that of the thiobenzamides.
D000410:Alanine Transaminase / Q000097:blood; D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D001219:Aspartate Aminotransferases / Q000097:blood; D001549:Benzamides / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D055598:Chemical Phenomena; D056486:Chemical and Drug Induced Liver Injury / Q000503:physiopathology*; D002627:Chemistry, Physical; D008297:Male; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity
D000995:Antitubercular Agents; D001549:Benzamides; D013844:Thiazoles; D001219:Aspartate Aminotransferases; D000410:Alanine Transaminase
Beziehungen zwischen chemischer Struktur, antituberkulotischer Aktivität und Hepatotoxizität von 2-Alkylthio-6-benzamidobenzothiazolen.