二芳基嘧啶类HIV-1非核苷类逆转录酶抑制剂研究进展  

Discovery and development of diarylpyrimidines (DAPYs) as next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs)

作　　者：田兴涛[1] 谢蓝[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《药学学报》2010年第2期177-183,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(20472114);北京市自然科学基金资助项目(7052057)

摘　　要：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 HIV-1 NNRTI drug Etravirine （TMC125） and a promising drug candidate Rilpivirine （TMC278） in phase III clinical trial are compounds belonging to the diarylpyrimidine （DAPY） family.They are extremely high potent against both wild-type and many drug-resistant HIV-1 strains,providing new hope for HIV-infected patients who fail to use current drugs due to the emergence of drug-resistant HIV mutants.The discovery and development of DAPY derivatives as next-generation NNRTI drugs depend on multidisciplinary coordination and their success has encouraged new researches to explore more next-generation NNRTIs with new scaffolds.This review described the story of discovery and development of DAPY derivatives as next-generation NNRTIs and related progress.

关 键 词：人类免疫缺陷病毒 非核苷类逆转录酶抑制剂 二芳基嘧啶类化合物 ETRAVIRINE Rilpivirine 

分 类 号：R978.7[医药卫生—药品]