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Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists.

作者信息

Paliwal Sunil, Reichard Gregory A, Shah Sapna, Wrobleski Michelle Laci, Wang Cheng, Stengone Carmine, Tsui Hon-Chung, Xiao Dong, Duffy Ruth A, Lachowicz Jean E, Nomeir Amin 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. 2008 Jul 15;18(14):4168-71. doi: 10.1016/j.bmcl.2008.05.082. Epub 2008 May 24.

DOI:10.1016/j.bmcl.2008.05.082
PMID:18547807
Abstract

Strategic replacement of the nitrogen of the lead compound 1 in the original cyclic urea series with a carbon resulted in the discovery of a novel, potent and orally more efficacious gamma-lactam series of selective NK(1) antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.

摘要

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