Discovery of a novel, potent and orally active series of gamma-lactams as selective NK1 antagonists期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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

Authors:	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

Affiliation:	^aChemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;^bCNS Biology Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;^cDepartment of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA

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 γ-lactam series of selective NK₁ antagonists. Optimization of the lactam series culminated in the identification of compounds with high binding affinity and excellent oral CNS activity.

Keywords:	NK1 Substance P Emesis CNS Lactam
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