强效gp120-CD4抑制剂的设计与优化。
Design and optimisation of potent gp120-CD4 inhibitors.
作者信息
Tran Thien-Duc, Adam Fiona M, Calo Frederick, Fenwick David R, Fok-Seang Juin, Gardner Iain, Hay Duncan A, Perros Manos, Rawal Jaiessh, Middleton Donald S, Parkinson Tanya, Pickford Christopher, Platts Michelle, Randall Amy, Stephenson Peter T, Vuong Hannah, Williams David H
机构信息
Discovery 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):5250-5. doi: 10.1016/j.bmcl.2009.06.102. Epub 2009 Jul 4.
The synthesis and structure-activity relationship of a series of novel gp120-CD4 inhibitors are described. Pharmacokinetic studies and antiviral spectrum assessment of lead compounds led to the identification of compound 36, a potent gp120-CD4 inhibitor which exhibited antiviral potency across a spectrum of 25 clade B isolates.
描述了一系列新型gp120-CD4抑制剂的合成及其构效关系。对先导化合物的药代动力学研究和抗病毒谱评估导致鉴定出化合物36，这是一种有效的gp120-CD4抑制剂，对25种B亚型分离株均表现出抗病毒活性。
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