新型非拟肽磺胺类HIV蛋白酶抑制剂Darunavir的研究进展

Progress in the New Generation Nonpeptide Sulfonamide Anti-HIV Protease Inhibitor Darunavir

综述新型非拟肽磺胺类人类免疫缺陷病毒(HIV)蛋白酶抑制剂Darunavir(TMC-114)的发现,抗病毒的活性,分子模拟以及结构优化的研究进展.Darunavir不但对野生型的HIV蛋白酶有很好的抑制活性,而且对多种抗性突变的HIV蛋白酶也有良好的活性,是针对耐药性HIV所开发的新药.

This article summarizes the discovery, activity, molecular mechanism and structural optimization of nonpeptide sulfonamide anti-HIV （human immunodeficienty virus） protease inhibitor darunavir （TMC-114）, which has not only a good inhibitory effect on wildtype HIV protease, but also fantastic inhibitory effects on many mutated HIV proteases, and is a new drug developed for HIV＇s resistance.