Design,Synthesis and Structure-Activity Relationships of N-Phenylarylformamide Derivatives（PAFAs） as Non-nucleoside HIV Reverse Transcriptase Inhibitors

作     者：Xiao-Dong Ma~a,Qiu-Qin He~a,Xuan Zhang~(b,c),Shi-Qiong Yang~a,Liu-Meng Yang~b,Shuang-Xi Gu~a, Yong-Tang Zheng~b,Fen-Er Chen~(a,d,*) a Department of Chemistry,Fudan University,Shanghai 200433,PR China b Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province,Kunming Institute of Zoology,Chinese Academy of Sciences,Kunming 650223,PR China c Graduate School of the Chinese Academy of Sciences,Beijing 100039,PR China d Institute of Biomedical Science,Fudan University,Shanghai 200031,PR China 

会议名称：《2011年全国药物化学学术会议——药物的源头创新》

会议日期：2011年

学科分类：1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学] 

摘      要：正A series of N-phenylarylformamide derivatives（PAFAs） with anti-wild-type HIV-1 EC50 values ranging from 0.3 nM to 5.1 nM and selectivity index values ranging from 10616 to 271000 were identified as novel non-nucleoside reverse transcriptase *** them,compound 13g （EC50 = 0.30 nM,SI = 184578）,131（EC50 = 0.37 nM,SI = 212819）,13m(EC50 = 0.32 nM,SI =