Cyclobutane derivatives as potent NK1 selective antagonists

Michelle Laci Wrobleski; Gregory A Reichard; Sunil Paliwal; Sapna Shah; Hon-Chung Tsui; Ruth A Duffy; Jean E Lachowicz; Cynthia A Morgan; Geoffrey B Varty; Neng-Yang Shih

doi:10.1016/j.bmcl.2006.04.031

Cyclobutane derivatives as potent NK1 selective antagonists

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3859-63. doi: 10.1016/j.bmcl.2006.04.031. Epub 2006 May 8.

Authors

Michelle Laci Wrobleski¹, Gregory A Reichard, Sunil Paliwal, Sapna Shah, Hon-Chung Tsui, Ruth A Duffy, Jean E Lachowicz, Cynthia A Morgan, Geoffrey B Varty, Neng-Yang Shih

Affiliation

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

PMID: 16682196
DOI: 10.1016/j.bmcl.2006.04.031

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.

MeSH terms

Animals
Binding Sites
Cyclobutanes / chemistry
Cyclobutanes / pharmacology*
Neurokinin-1 Receptor Antagonists*
Serotonin Antagonists / chemistry*
Serotonin Antagonists / pharmacology*
Stereoisomerism
Structure-Activity Relationship

Substances

Cyclobutanes
Neurokinin-1 Receptor Antagonists
Serotonin Antagonists