Identification of Novel Diarylpyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors against Wild-Type and K103N Mutant Viruses
Xiangyi Jiang,Waleed A. Zalloum,Zhen Gao,Jiaojiao Dai,Xiangkai Ji,Minghui Xie,Guanyu Dong,Erik De Clercq,Boshi Huang,Christophe Pannecouque,Peng Zhan,Xinyong Liu
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 mutant strains with EC