Department of Chemistry, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, R.R. District 500078, Andhra Pradesh, India.
Bioorg Med Chem Lett. 2013 Dec 15;23(24):6805-10. doi: 10.1016/j.bmcl.2013.10.016. Epub 2013 Oct 14.
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.
这封信的重点是设计和合成一系列十九个新的 6-(4-((取代-1H-1,2,3-三唑-4-基)甲基)哌嗪-1-基)菲啶类似物，采用点击化学方法，并评估它们对结核分枝杆菌 H37Rv 的抗结核活性。在所测试的化合物中，7f 和 7j 表现出良好的活性（MIC = 3.125 μg/mL），而 8a 对结核分枝杆菌 H37Rv 的生长表现出优异的活性（MIC = 1.56 μg/mL）。此外，化合物 7f、7j 和 8a 还进行了对小鼠巨噬细胞（RAW264.7）细胞系的细胞毒性研究，其选择性指数值>15，表明这些化合物适合进一步的药物开发。
