【摘 要】
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In order to improve the positional adaptability of our previously reported naphthyl diaryltria-zines (NP-DATAs),synthesis of a series of novel biphenyl-substitu
【机 构】
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Engineering Center of Catalysis and Synthesis for Chiral Molecules,Department of Chemistry,Fudan Uni
论文部分内容阅读
In order to improve the positional adaptability of our previously reported naphthyl diaryltria-zines (NP-DATAs),synthesis of a series of novel biphenyl-substituted diaryltriazines (BP-DATAs) with a flexible side chain attached at the C-6 position is presented.These compounds exhibited excellent potency against wild-type (WT) HIV-1 with EC5o values ranging from 2.6 to 39 nmol/L and most of them showed low nanomolar anti-viral potency against a panel of HIV-1 mutant strains.Compounds 5j and 6k had the best activity against WT,single and double HIV-1 mutants and reverse transcriptase (RT) enzyme comparable to two reference drugs (EFV and ETR) and our lead compound NP-DATA (1).Molecular modeling disclosed that the side chain at the C-6 position of DATAs occupied the entrance channel of the HIV-1 reverse transcriptase non-nucleoside binding pocket (NNIBP) attributing to the improved activity.The preliminary structure-activity relationship and PK profiles were also discussed.
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