Zhan Peng, Li Zhenyu, Liu Xinyong, De Clercq Erik
Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, 250012, Jinan, Shandong, P.R.China.
Mini Rev Med Chem. 2009 Jul;9(8):1014-23. doi: 10.2174/138955709788681618.
There is an urgent need for the design and development of new and safer drugs for the treatment of human immunodeficiency virus (HIV) infection, specifically active against drug-resistant viral strains. Recently, sulfanyltriazole/tetrazole derivatives were reported as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), with low nanomolar intrinsic activity against RT and submicromolar antiviral activity in HIV infected cells. In this review, the structural modifications, SAR analysis and docking studies of sulfanyltriazole/tetrazoles HIV-1 NNRTIs are discussed, and other interesting NNRTIs with the same or similar pharmacophore as the sulfanyltriazole/tetrazole derivatives are also presented and analyzed for their in SAR.
迫切需要设计和开发用于治疗人类免疫缺陷病毒（HIV）感染的新型更安全药物，特别是对耐药病毒株具有活性的药物。最近，硫烷基三唑/四唑衍生物被报道为有效的HIV-1非核苷类逆转录酶抑制剂（NNRTIs），对逆转录酶具有低纳摩尔内在活性，在HIV感染细胞中具有亚微摩尔抗病毒活性。在本综述中，讨论了硫烷基三唑/四唑类HIV-1 NNRTIs的结构修饰、构效关系（SAR）分析和对接研究，还介绍并分析了其他与硫烷基三唑/四唑衍生物具有相同或相似药效团的有趣NNRTIs的构效关系。
