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本文以吡啶酮类逆转录酶抑制剂和二酮酸类(DKA)整合酶抑制剂为先导化合物,选取必要的药效团进行高度整合并对其进行合理优化,设计出的三个系列的HIV-1 RT/IN双靶点抑制剂.采用表面等离子共振(SPR)技术及酶联免疫吸附法对目标化合物分别进行了体外抗HIV-1 RT和IN的生物活性测定.实验结果表明,化合物A2对逆转录酶和整合酶都表现出较好的抑制活性,为深入研究该类化合物作为HIV-l双靶点抑制剂提供了相关信息.“,”Three series of novel anti-immunodeficiency virus 1 (H1V-1) dual (RT/IN) inhibitors were rationally designed by introducing a functioning diketo acid (DKA) into pyridin-2-one scaffold.To efficiently analyze inhibitory activity,these compounds were screened against HIV-1 RT and IN respectively via surface plasmon resonance (SPR),and active compounds were subsequently evaluated by enzyme assay.It was noteworthy that compound A2 exhibited moderate activity against both HIV-1 RT and IN.This result provided information for further development ofpyridinone analogues as potent dual HIV-1 inhibitors.