Design,synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents |
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Authors: | Hunsur Nagendra Nagesh Kalaga Mahalakshmi Naidu Damarla Harika Rao Jonnalagadda Padma Sridevi Dharmarajan Sriram Perumal Yogeeswari Kondapalli Venkata Gowri Chandra Sekhar |
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Institution: | 1. Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District 500078, Andhra Pradesh, India;2. Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District 500078, Andhra Pradesh, India |
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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 7j 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, 7j 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. |
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Keywords: | Phenanthridine Piperazine Triazole Click chemistry Anti-tubercular activity |
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