Article
Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses.
Bioorganic & medicinal chemistry - 15 Jul 2021
Fu Zhipeng, Zhang Tao, Zhou Zhongxia, Kang Dongwei, Sun Lin, Gao Shenghua, Cherukupalli Srinivasulu, De Clercq Erik, Pannecouque Christophe, Liu Xinyong, Zhan Peng
Abstract excerpt
To further explore the chemical space surrounding the "hydrophobic channel" of the NNRTI binding pocket (NNIBP), a new series of diarylpyrimidines (DAPYs) were designed and synthesized as potent HIV-1 non-nucleoside RT inhibitors (NNRTIs). The target compounds were evaluated for anti-HIV potency in MT-4 cells. Most of the synthesized DAPYs exhibited moderate to excellent activity against the HIV-1 wild-type (WT)...
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