Article
Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.
European journal of medicinal chemistry - 6 Oct 2014
Wang Liu, Tian Ye, Chen Wenmin, Liu Hong, Zhan Peng, Li Dongyue, Liu Huiqing, De Clercq Erik, Pannecouque Christophe, Liu Xinyong
Abstract excerpt
Guided by crystal structures of HIV-1 RT/DAPY complex and molecular modeling studies, a series of novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives were rationally designed via structure-based core refining approach, synthesized through the readily accessible synthetic methods and evaluated for their anti-HIV activities in MT-4 cells. Preliminary biological evaluation indicated that most of the compounds...
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