Article
Identification of novel diarylpyrimidine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors against wild-type and K103N mutant viruses.
European journal of medicinal chemistry - 15 Dec 2024
Jiang Xiangyi, Zalloum Waleed A, Gao Zhen, Dai Jiaojiao, Ji Xiangkai, Xie Minghui, Dong Guanyu, De Clercq Erik, Huang Boshi, Pannecouque Christophe, Zhan Peng, Liu Xinyong
Abstract excerpt
HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) play a crucial role in combination antiretroviral therapy (cART). To further enhance their antiviral activity and anti-resistance properties, we developed a series of novel NNRTIs, by specifically targeting tolerant region I of the NNRTI binding pocket. Among them, compound 9t-2 displayed excellent anti-HIV-1 potency against wild-type and prevalent...
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