Article
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
Journal of medicinal chemistry - 8 Sept 2016
Kang Dongwei, Fang Zengjun, Li Zhenyu, Huang Boshi, Zhang Heng, Lu Xueyi, Xu Haoran, Zhou Zhongxia, Ding Xiao, Daelemans Dirk, De Clercq Erik, Pannecouque Christophe, Zhan Peng, Liu Xinyong
Abstract excerpt
We designed and synthesized a series of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) with a piperidine-substituted thiophene[3,2-d]pyrimidine scaffold, employing a strategy of structure-based molecular hybridization and substituent decorating. Most of the synthesized compounds exhibited broad-spectrum activity with low (single-digit) nanomolar EC50 values...
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