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2008年FDA批准上市的新一代非核苷类逆转录酶抑制剂Etravirine(TMC125)和Ⅲ期临床候选药Rilpivirine(TMC278)都是二芳基嘧啶(DAPY)类化合物,均对HIV野生型和多种耐药性病毒株有相当强的抑制作用。DAPY类药物的发现和发展是多学科合作研发新药的成功范例。本文综述了新一代HIV非核苷类逆转录酶抑制剂DAPY类化合物的发现、发展及最新研究进展。
The new generation of non-nucleoside reverse transcriptase inhibitors Etravirine (TMC125) and Phase III clinical candidate Rilpivirine (TMC278) approved by the FDA in 2008 are diarylpyrimidines (DAPYs), both of which are active against HIV wild type and multiple Drug-resistant virus strains have a very strong inhibitory effect. The discovery and development of DAPY drugs is a successful example of multidisciplinary cooperation in research and development of new drugs. This review summarizes the discovery, development and recent research progress of the new generation of non-nucleoside reverse transcriptase inhibitor DAPY.