| Title | Synthesis and biological evaluation of imidazole thioacetanilides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. | | Author(s) | Zhan P, Liu X, Zhu J, Fang Z, Li Z, Pannecouque C, Clercq ED | | Institution | Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, No. 44 Wenhuaxi Road, Jinan 250012, PR China. | | Source | Bioorg Med Chem 2009 Jul 18. | | 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 (EC(50)=0.18muM), and 4a2 (EC(50)=0.20muM), which were more effective than the lead compound L1 (EC(50)=2.053muM) and the reference drugs nevirapine and delavirdine. The preliminary structure-activity relationship (SAR) of the newly synthesized congeners is discussed. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19643613 |
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