A convenient synthesis and screening of benzosuberone bearing 1, 2, 3-triazoles against Mycobacterium tuberculosis. Issue 17 (1st September 2016)

• Record Type: Journal Article
• Authors: Sajja, Yasodakrishna; Vanguru, Sowmya; Jilla, Lavanya; Vulupala, Hanmanth Reddy; Bantu, Rajashaker; Yogeswari, Perumal; Sriram, Dharmarajan; Nagarapu, Lingaiah
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 17(2016)
• Page Start: 4292
• Page End: 4295
• Publication Date: 2016-09-01
• Subjects: Benzosuberone -- Triazole -- Reduction -- Antitubercular agents -- Click chemistry; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.07.039
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: A series of benzosuberone bearing 1, 2, 3-triazoles have been synthesized and screened for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Compounds5h (MIC: 3.125 μg/mL) and5l, 5m, 5o (MIC: 6.25 μg/mL) exhibited promising hits. Abstract: A series of benzosuberone bearing 1, 2, 3-triazoles were rationally designed and alkyl/aryl groups appended on 1, 2, 3-triazole derivatives5a –o were synthesized using click chemistry and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC27294). Compounds5h (MIC: 3.125 μg/mL) and5l, 5m, 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.