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

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 H(37)Rv. Among the tested compounds, 7f and 7j exhibited good activity (MIC = 3.125 mu g/mL), while 8a displayed excellent activity (MIC = 1.56 mu g/mL) against the growth of M. tuberculosis H(37)Rv. 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. (C) 2013 Elsevier Ltd. All rights reserved.