Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent

Alan Brown; Lindsay Brown; T Bruce Brown; Andrew Calabrese; Dave Ellis; Nicholas Puhalo; Chris R Smith; Olga Wallace; Lesa Watson

doi:10.1016/j.bmcl.2008.08.066

Triazole oxytocin antagonists: identification of aryl ether replacements for a biaryl substituent

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5242-4. doi: 10.1016/j.bmcl.2008.08.066. Epub 2008 Aug 22.

Authors

Alan Brown¹, Lindsay Brown, T Bruce Brown, Andrew Calabrese, Dave Ellis, Nicholas Puhalo, Chris R Smith, Olga Wallace, Lesa Watson

Affiliation

¹ Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. Alan.D.Brown@pfizer.com

PMID: 18778939
DOI: 10.1016/j.bmcl.2008.08.066

Abstract

Several potent aryl ether/triazole oxytocin antagonists are described. The lead compound in this series had significantly improved aqueous solubility over related systems containing a biaryl substituent.

MeSH terms

Administration, Oral
Animals
Molecular Structure
Oxytocin / antagonists & inhibitors*
Rats
Structure-Activity Relationship
Triazoles / chemical synthesis*
Triazoles / chemistry
Triazoles / pharmacology*

Substances

Triazoles
Oxytocin