Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors |
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| Authors: | Peng Zhan Xinyong Liu Junjie Zhu Zengjun Fang Zhenyu Li Christophe Pannecouque Erik De Clercq |
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| Affiliation: | 1. Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012, PR China;2. Rega Institute for Medical Research, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium |
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| Abstract: | A series of 2-(1-aryl-1H-imidazol-2-ylthio)acetamide [imidazole thioacetanilide (ITA)] derivatives were synthesized and evaluated as potent inhibitors of human immunodeficiency virus type-1 (HIV-1). Among them, the most potent HIV-1 inhibitors were 4a5 (EC50 = 0.18 μM), and 4a2 (EC50 = 0.20 μM), which were more effective than the lead compound L1 (EC50 = 2.053 μM) and the reference drugs nevirapine and delavirdine. The preliminary structure–activity relationship (SAR) of the newly synthesized congeners is discussed. |
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