The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists

Susan Napier; Grant Wishart; William Arbuckle; James Baker; David Barn; Matilda Bingham; Angus Brown; Alan Byford; Chris Claxton; Mark Craighead; Kirsteen Buchanan; Lee Fielding; Lindsay Gibson; Richard Goodwin; Susan Goutcher; Nicholas Irving; Cliona MacSweeney; Rachel Milne; Chris Mort; Jeremy Presland; Hazel Sloan; Fiona Thomson; Zara Turnbull; Trevor Young

doi:10.1016/j.bmcl.2011.02.096

The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists

Bioorg Med Chem Lett. 2011 May 15;21(10):3163-7. doi: 10.1016/j.bmcl.2011.02.096. Epub 2011 Mar 4.

Affiliation

¹ Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK. susannapier67@googlemail.com

PMID: 21458261
DOI: 10.1016/j.bmcl.2011.02.096

Abstract

The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. Compounds 47 and 48 were found to be high affinity, selective vasopressin V(1A) antagonists.

MeSH terms

Amides / chemical synthesis*
Amides / chemistry
Amides / pharmacology*
Antidiuretic Hormone Receptor Antagonists*
Aza Compounds / chemical synthesis
Aza Compounds / chemistry
Aza Compounds / pharmacology
Cells, Cultured
Cyclization
Drug Discovery*
Humans
Liver / metabolism
Molecular Structure
Protein Binding / drug effects

Substances

Amides
Antidiuretic Hormone Receptor Antagonists
Aza Compounds