Design, synthesis and activity evaluation of novel pyridinone derivatives as anti-HIV-1 dual(RT/IN) inhibitors

作     者：Quanzhi Yang Tao Sheng Ningning Fan Yameng Hao Yuanyuan Cao Ying Guo Zhili Zhang Chao Tian Junyi Liu Xiaowei Wang 杨全志;盛涛;樊宁宁;郝亚萌;曹源源;郭莹;张志丽;田超;刘俊义;王孝伟

作者机构：Department of Chemical Biology School of Pharmaceutical Sciences Peking University Health Science Center Beijing 100191 China 

基　　金：National Natural Science Foundation of China(Grant No.21172014,812111023 and 81172733) grants from the Ministry of Science and Technology of China(Grant No.200 9ZX09301-010) 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2017年第26卷第1期

页      码：31-44页

摘      要：Three series of novel anti-immunodeficiency virus 1 （HIV-1） dual （RT/1N） inhibitors were rationally designed by introducing a functioning diketo acid （DKA） into pyridin-2-one scaffold. To efficiently analyze inhibitory activity, these compounds were screened against HIV-1 RT and IN respectively via surface plasmon resonance （SPR）, and active compounds were subsequently evaluated by enzyme assay. It was noteworthy that compound A2 exhibited moderate activity against both HIV-1 RT and IN. This result provided information for further development of pyridinone analogues as potent dual HIV-1 inhibitors.

主 题 词：Pyridinone derivatives HIV-1 dual inhibitor Reverse transcriptase Integrase 

学科分类：1007[医学-药学类] 10[医学] 100701[100701] 

核心收录：

D　O　I：10.5246/jcps.2017.01.003

馆 藏 号：203211139...