Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor

Jason Witherington; Lee Abberley; Benjamin R Bellenie; Rio Boatman; Katharine Collis; David K Dean; Alessandra Gaiba; N Paul King; Nicola Shuker; Jon G A Steadman; Andrew K Takle; Gareth Sanger; Sharon Butler; Fiona McKay; Alison Muir; Kim Winborn; Robert W Ward; Tom D Heightman

doi:10.1016/j.bmcl.2008.12.042

Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor

Bioorg Med Chem Lett. 2009 Feb 1;19(3):684-7. doi: 10.1016/j.bmcl.2008.12.042. Epub 2008 Dec 14.

Authors

Jason Witherington¹, Lee Abberley, Benjamin R Bellenie, Rio Boatman, Katharine Collis, David K Dean, Alessandra Gaiba, N Paul King, Nicola Shuker, Jon G A Steadman, Andrew K Takle, Gareth Sanger, Sharon Butler, Fiona McKay, Alison Muir, Kim Winborn, Robert W Ward, Tom D Heightman

Affiliation

¹ Department of Medicinal Chemistry & DMPK, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Jason_Witherington@GSK.com

PMID: 19128969
DOI: 10.1016/j.bmcl.2008.12.042

Abstract

As part of an on-going lead optimisation effort, a cross screening exercise identified an aryl sulphonyl amide hit that was optimised to afford a highly potent series of ghrelin receptor agonists.

MeSH terms

Administration, Oral
Animals
Biological Availability
Chemistry, Pharmaceutical / methods*
Drug Design
Ghrelin / chemistry*
Growth Hormone / chemistry
Male
Models, Chemical
Protein Processing, Post-Translational
Rats
Rats, Sprague-Dawley
Receptors, Ghrelin / antagonists & inhibitors*
Receptors, Ghrelin / chemistry
Structure-Activity Relationship
Sulfones / chemistry*

Substances

Ghrelin
Receptors, Ghrelin
Sulfones
Growth Hormone