论文部分内容阅读
整合酶(integrase,IN)是人类免疫缺陷1型病毒(human immunodeficiency virus-1,HIV-1)复制过程必需的酶,而人类细胞中没有该酶的类似物,理论上抑制IN对人体副作用很小,因此HIV-1IN成为治疗艾滋病(acquired immunodeficiency syndrome,AIDS)合理的靶点。本文综述了近年来α,γ-二酮类IN抑制剂的发展现状,为发展定量构效关系(quantitative structure-activity relationship,QSAR)、进行虚拟筛选、确认药效团假说和指导合成活性更高的IN抑制剂提供参考。
Integrase (IN) is an essential enzyme for the replication of human immunodeficiency virus-1 (HIV-1), but there is no analogue of this enzyme in human cells. Theoretically, the side effects of IN on human body are very poor HIV-1IN is therefore a reasonable target for acquired immunodeficiency syndrome (AIDS). This review summarizes the recent development of IN inhibitors of α, γ-diketones. In order to develop a quantitative structure-activity relationship (QSAR), we conducted a virtual screening to confirm the pharmacophore hypothesis and guide the higher synthetic activity IN inhibitors for reference.