Cyclobutane derivatives as potent NK1 selective antagonists.
作者信息
Wrobleski Michelle Laci, Reichard Gregory A, Paliwal Sunil, Shah Sapna, Tsui Hon-Chung, Duffy Ruth A, Lachowicz Jean E, Morgan Cynthia A, Varty Geoffrey B, Shih Neng-Yang
机构信息
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jul 15;16(14):3859-63. doi: 10.1016/j.bmcl.2006.04.031. Epub 2006 May 8.
PMID:16682196
Abstract
A series of novel cyclobutane derivatives as potent and selective NK1 receptor antagonists is described. Several compounds in this series exhibited high in vitro binding affinity (Ki <or=1 nM), and potent inhibition of central NK1 receptor following oral administration. Syntheses of these compounds are also described herein.
摘要
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