The characterization of a novel V1b antagonist lead series

Chris A Smethurst; Jennifer A Borthwick; Simon Gaines; Steve Watson; Andrew Green; Mark J Schulz; George Burton; Alberto A Buson; Roberto Arban

doi:10.1016/j.bmcl.2010.11.061

The characterization of a novel V1b antagonist lead series

Bioorg Med Chem Lett. 2011 Jan 1;21(1):92-6. doi: 10.1016/j.bmcl.2010.11.061. Epub 2010 Nov 19.

Authors

Chris A Smethurst¹, Jennifer A Borthwick, Simon Gaines, Steve Watson, Andrew Green, Mark J Schulz, George Burton, Alberto A Buson, Roberto Arban

Affiliation

¹ GlaxoSmithKline Research and Development, New Frontiers Science Park, Harlow, UK.

PMID: 21146408
DOI: 10.1016/j.bmcl.2010.11.061

Abstract

The SAR around a V1b antagonist HTS hit 3 was explored to produce a series of thiazole sulfonamides as a lead series with selectivity over the related V1 and oxytocin receptors.

MeSH terms

Animals
Antidiuretic Hormone Receptor Antagonists*
High-Throughput Screening Assays
Rats
Receptors, Oxytocin / antagonists & inhibitors
Receptors, Oxytocin / metabolism
Receptors, Vasopressin / metabolism
Structure-Activity Relationship
Sulfonamides / chemistry*
Thiazoles / chemistry

Substances

Antidiuretic Hormone Receptor Antagonists
Receptors, Oxytocin
Receptors, Vasopressin
Sulfonamides
Thiazoles