Article
Targeting dual tolerant regions of binding pocket: Discovery of novel morpholine-substituted diarylpyrimidines as potent HIV-1 NNRTIs with significantly improved water solubility.
European journal of medicinal chemistry - 15 Nov 2020
Wang Zhao, Kang Dongwei, Feng Da, Cherukupalli Srinivasulu, Jiang Xiangyi, Fu Zhipeng, De Clercq Erik, Pannecouque Christophe, Liu Xinyong, Zhan Peng
Abstract excerpt
To address the intractable issues of drug resistance and poor solubility, a novel series of morpholine-substituted diarylpyrimidines targeting the tolerant region I and tolerant region II of NNIBP were rationally designed by utilizing the available crystallography studies. The biological evaluation results showed that four most promising compounds (14e1, 14g1, 14g2 and 14j2) displayed excellent potency against WT...
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