通过干扰gp120与CD4的相互作用发现一种小分子抑制剂。
Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction.
作者信息
Williams David H, Adam Fiona, Fenwick David R, Fok-Seang Juin, Gardner Iain, Hay Duncan, Jaiessh Rawal, Middleton Donald S, Mowbray Charles E, Parkinson Tanya, Perros Manos, Pickford Christopher, Platts Michelle, Randall Amy, Siddle Daniel, Stephenson Peter T, Tran Thien-Duc, Vuong Hannah
机构信息
Department of Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, UK.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5246-9. doi: 10.1016/j.bmcl.2009.06.080. Epub 2009 Jun 25.
A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.
设计并合成了一系列哌嗪衍生物作为gp120-CD4抑制剂。构效关系研究导致在以化合物9和28为代表的基于细胞的抗病毒试验中发现了强效抑制剂。还介绍了所选化合物的大鼠药代动力学和抗病毒概况。
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