title: Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.
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.
authors.affiliation: 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
authors.forename: Jason
authors.initials: J
authors.lastname: Witherington
authors.forename: Lee
authors.initials: L
authors.lastname: Abberley
authors.forename: Benjamin R
authors.initials: BR
authors.lastname: Bellenie
authors.forename: Rio
authors.initials: R
authors.lastname: Boatman
authors.forename: Katharine
authors.initials: K
authors.lastname: Collis
authors.forename: David K
authors.initials: DK
authors.lastname: Dean
authors.forename: Alessandra
authors.initials: A
authors.lastname: Gaiba
authors.forename: N Paul
authors.initials: NP
authors.lastname: King
authors.forename: Nicola
authors.initials: N
authors.lastname: Shuker
authors.forename: Jon G A
authors.initials: JG
authors.lastname: Steadman
authors.forename: Andrew K
authors.initials: AK
authors.lastname: Takle
authors.forename: Gareth
authors.initials: G
authors.lastname: Sanger
authors.forename: Sharon
authors.initials: S
authors.lastname: Butler
authors.forename: Fiona
authors.initials: F
authors.lastname: McKay
authors.forename: Alison
authors.initials: A
authors.lastname: Muir
authors.forename: Kim
authors.initials: K
authors.lastname: Winborn
authors.forename: Robert W
authors.initials: RW
authors.lastname: Ward
authors.forename: Tom D
authors.initials: TD
authors.lastname: Heightman
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D054439:Ghrelin / Q000737:chemistry*; D013006:Growth Hormone / Q000737:chemistry; D008297:Male; D008956:Models, Chemical; D011499:Protein Processing, Post-Translational; D051381:Rats; D017207:Rats, Sprague-Dawley; D054440:Receptors, Ghrelin / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry*
chemical_list: D054439:Ghrelin; D054440:Receptors, Ghrelin; D013450:Sulfones; D013006:Growth Hormone