Sriram Dharmarajan, Srichakravarthy Narasimharaghavan, Bal Tanushree R, Yogeeswari Perumal
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India.
Biomed Pharmacother. 2005 Sep;59(8):456-9. doi: 10.1016/j.biopha.2005.07.010.
A series of nevirapine derivatives has been synthesized in an effort to enhance the spectrum of chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. The nevirapine derivative bearing isoniazid moiety (3a) was found to be the most potent compound with EC50 of<0.0636 microM, CC50 of>1000 microM and selectivity index of>15,723 which also exhibited 90% inhibition against Mycobacterium tuberculosis at 6.25 microg/ml. Compound 3c showed 100% inhibition against M. tuberculosis and also exhibited potent antibacterial activity against 24 pathogenic bacteria with MIC less than 1 microg/ml.
为了增强化疗特性谱以有效治疗艾滋病及与艾滋病相关的机会性感染，已合成了一系列奈韦拉平衍生物。发现带有异烟肼部分的奈韦拉平衍生物（3a）是最有效的化合物，其半数有效浓度（EC50）<0.0636微摩尔，半数细胞毒性浓度（CC50）>1000微摩尔，选择性指数>15723，并且在6.25微克/毫升时对结核分枝杆菌也表现出90%的抑制作用。化合物3c对结核分枝杆菌表现出100%的抑制作用，并且对24种病原菌也表现出强效抗菌活性，其最低抑菌浓度（MIC）小于1微克/毫升。
