Article
Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue.
European journal of medicinal chemistry - 18 Sept 2015
Wan Zheng-Yong, Yao Jin, Mao Tian-Qi, Wang Xin-Long, Wang Hai-Feng, Chen Wen-Xue, Yin Hong, Chen Fen-Er, De Clercq Erik, Daelemans Dirk, Pannecouque Christophe
Abstract excerpt
Based on molecular simulation, the etravirine-VRX-480773 hybrids previously disclosed by our group were optimized to yield novel pyrimidine sulfonylacetanilides 8 with improved activity against a panel of seven clinically relevant single and double mutant strains of HIV-1. The improvement in potency in this in vitro model of HIV RNA replication partly validates the mechanism by which this class of allosteric...
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