A convenient synthesis and screening of benzosuberone bearing 1,2,3-triazoles against Mycobacterium tuberculosis

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• 作者：Yasodakrishna Sajja^a ; Sowmya Vanguru^a ; Lavanya Jilla^a ; Hanmanth Reddy Vulupala^a ; Rajashaker Bantu^a ; Perumal Yogeswari^b ; Dharmarajan Sriram^b ; Lingaiah Nagarapu^a ; ^{lnagarapuiict@yahoo.com" class="auth_mail" title="E-mail the corresponding author} ; ^{nagarapu@iict.res.in" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Benzosuberone ; Triazole ; Reduction ; Antitubercular agents ; Click chemistry
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 September 2016
• 年：2016
• 卷：26
• 期：17
• 页码：4292-4295
• 全文大小：780 K

文摘

A series of benzosuberone bearing 1,2,3-triazoles were rationally designed and alkyl/aryl groups appended on 1,2,3-triazole derivatives boldFont">5a–boldFont">o were synthesized using click chemistry and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC27294). Compounds boldFont">5h (MIC: 3.125 μg/mL) and boldFont">5l, boldFont">5m, boldFont">5o (MIC: 6.25 μg/mL) exhibited promising hits. This is the first Letter on the synthesis and in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv of benzosuberone alkyl/aryl groups appended on 1,2,3-triazole derivatives.