Structure‐based design of diarylpyrimidines and triarylpyrimidines as potent HIV‐1 NNRTIs with improved metabolic stability and drug resistance profiles
Minghui Xie,
Zhao Wang,
Fabao Zhao
et al.
Abstract:Non‐nucleoside reverse transcriptase inhibitors (NNRTIs) are an important component of anti‐acquired immunodeficiency syndrome treatment regimen. In the present work, with the previously reported compound K‐16c as lead, a series of novel 2,4,5‐trisubstituted pyrimidine derivatives were designed based on the cocrystal structure of K‐16c/RT, with the aim to improve the anti‐human immunodeficiency virus type‐1 (HIV‐1) activities and metabolic stability properties. Compound 11b1 exhibited the most potent antiviral… Show more
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