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

作者：Sajja Yasodakrishna; Vanguru Sowmya; Jilla Lavanya; Vulupala Hanmanth Reddy; Bantu Rajashaker; Yogeswari Perumal; Sriram Dharmarajan; Nagarapu Lingaiah^*

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(17): 4292-4295.

DOI：10.1016/j.bmcl.2016.07.039

• Benzosuberone
• Triazole
• Reduction
• Antitubercular agents
• Click chemistry

A series of benzosuberone bearing 1,2,3-triazoles were rationally designed and alkyl/aryl groups appended on 1,2,3-triazole derivatives 5a-o were synthesized using click chemistry and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC27294). Compounds 5h (MIC: 3.125 mu g/mL) and 51, 5m, 5o (MIC: 6.25 mu g/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.

• 出版日期2016-9-1