Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.

Xuwang Chen,Xin Liu,Qing Meng,Ding Wang,Huiqing Liu,Erik De Clercq,Christophe Pannecouque,Jan Balzarini,Xinyong Liu

Bioorganic & Medicinal Chemistry Letters（2013）

引用 27|浏览9

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摘要

Compound 10b3 (EC50=0.047 (wild-type) and 4.6μM (mutant)) with dual structural conformations was designed via molecular hybridization, and could occupy the protein/solvent interface and the entrance channel of HIV-1 NNIBP simultaneously.

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关键词

HIV-1 NNRTIs,DAPY,Piperidin-4-yl-aminopyrimidines,Dual conformations,Molecular hybridization

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