S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents

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• 作者：Galina Karabanovich^a ; Jan Němeček^a ; Lenka Val&aacute ; &scaron ; kov&aacute ; ^a ; Alejandro Carazo^a ; Kl&aacute ; ra Konečn&aacute ; ^a ; Jiřina Stolaří ; kov&aacute ; ^b ; Alexandr Hrab&aacute ; lek^a ; Oto Pavli&scaron ; ^c ; Petr P&aacute ; vek^a ; Kateřina V&aacute ; vrov&aacute ; ^a ; Jaroslav Roh^a ; ^{jaroslav.roh@faf.cuni.cz} ; Věra Klime&scaron ; ov&aacute ; ^a
• 关键词：Tuberculosis ; Antitubercular agent ; Mycobacterium tuberculosis ; Tetrazole ; Oxadiazole ; Structure-activity relationships
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：369-383
• 全文大小：1487 K
• 卷排序：126

文摘

3,5-Dinitrophenyl tetrazoles and oxadiazoles with high antimycobacterial activity. MIC values of 0.03–0.06 μM against Mycobacterium tuberculosis. Activity against MDR/XDR strains and no cross-resistance with common anti-TB drugs. Selective antitubercular effect and low in vitro toxicity to mammalian cell lines. Defined structure-activity relationships.