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. 2013 Dec 15;23(24):6805-10.
doi: 10.1016/j.bmcl.2013.10.016. Epub 2013 Oct 14.

Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents

Hunsur Nagendra Nagesh  1 , Kalaga Mahalakshmi Naidu, Damarla Harika Rao, Jonnalagadda Padma Sridevi, Dharmarajan Sriram, Perumal Yogeeswari, Kondapalli Venkata Gowri Chandra Sekhar
Affiliations

Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents

Hunsur Nagendra Nagesh et al. Bioorg Med Chem Lett. .

Abstract

Focus in this Letter is made to design and synthesize a series of nineteen new 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues employing click chemistry and evaluated for their anti-tubercular activity against Mycobacterium tuberculosis H37Rv. Among the tested compounds, 7f and 7 j exhibited good activity (MIC = 3.125 μg/mL), while 8a displayed excellent activity (MIC = 1.56 μg/mL) against the growth of M. tuberculosis H37Rv. In addition, 7f, 7 j and 8a compounds were subjected to cytotoxic studies against mouse macrophage (RAW264.7) cell lines and the selectivity index values are >15 indicating suitability of compounds for further drug development.

Keywords: Anti-tubercular activity; Click chemistry; Phenanthridine; Piperazine; Triazole.

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