人CCR5趋化因子受体的4-（杂芳基哌啶-1-基-甲基）-吡咯烷-1-基-乙酸拮抗剂的合成及构效关系研究
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
作者信息
Shankaran K, Donnelly Karla L, Shah Shrenik K, Guthikonda Ravindra N, MacCoss Malcolm, Mills Sander G, Gould Sandra L, Malkowitz Lorraine, Siciliano Salvatore J, Springer Martin S, Carella Anthony, Carver Gwen, Hazuda Daria, Holmes Karen, Kessler Joseph, Lineberger Janet, Miller Michael D, Emini Emilio A, Schleif William A
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2004 Jul 5;14(13):3419-24. doi: 10.1016/j.bmcl.2004.04.078.
Efforts toward the exploration of the title compounds as CCR5 antagonists are disclosed. The basis for such work stems from the fact that cellular proliferation of HIV-1 requires the cooperative assistance of both CCR5 and CD4 receptors. The synthesis and SAR of pyrrolidineacetic acid derivatives as CCR5 antagonists displaying potent binding and antiviral properties in a HeLa cell-based HIV-1 infectivity assay are discussed.
本文公开了探索标题化合物作为CCR5拮抗剂的研究工作。开展此类研究的依据是，HIV-1的细胞增殖需要CCR5和CD4受体的协同作用。文中讨论了吡咯烷乙酸衍生物作为CCR5拮抗剂的合成及其构效关系，这些衍生物在基于HeLa细胞的HIV-1感染性试验中表现出强效结合和抗病毒特性。
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