Cyclic urea derivatives as potent NK1 selective antagonists

Ho-Jane Shue; Xiao Chen; Neng-Yang Shih; David J Blythin; Sunil Paliwal; Ling Lin; Danlin Gu; John H Schwerdt; Sapna Shah; Gregory A Reichard; John J Piwinski; Ruth A Duffy; Jean E Lachowicz; Vicki L Coffin; Fei Liu; Amin A Nomeir; Cynthia A Morgan; Geoffrey B Varty

doi:10.1016/j.bmcl.2005.05.111

Cyclic urea derivatives as potent NK1 selective antagonists

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3896-9. doi: 10.1016/j.bmcl.2005.05.111.

Authors

Ho-Jane Shue¹, Xiao Chen, Neng-Yang Shih, David J Blythin, Sunil Paliwal, Ling Lin, Danlin Gu, John H Schwerdt, Sapna Shah, Gregory A Reichard, John J Piwinski, Ruth A Duffy, Jean E Lachowicz, Vicki L Coffin, Fei Liu, Amin A Nomeir, Cynthia A Morgan, Geoffrey B Varty

Affiliation

¹ Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

PMID: 16019209
DOI: 10.1016/j.bmcl.2005.05.111

Abstract

A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists. Several compounds in this series exhibited good oral activity and brain penetration. Syntheses of these compounds are also described herein.

MeSH terms

Animals
Biological Availability
Dose-Response Relationship, Drug
Gerbillinae
Heterocyclic Compounds / chemical synthesis
Heterocyclic Compounds / pharmacokinetics
Heterocyclic Compounds / pharmacology
Motor Activity / drug effects
Neurokinin-1 Receptor Antagonists*
Protein Binding
Rats
Structure-Activity Relationship
Urea / analogs & derivatives*
Urea / pharmacokinetics
Urea / pharmacology

Substances

Heterocyclic Compounds
Neurokinin-1 Receptor Antagonists
Urea