Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.
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.
Witherington
Jason
J
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
Abberley
Lee
L
Bellenie
Benjamin R
BR
Boatman
Rio
R
Collis
Katharine
K
Dean
David K
DK
Gaiba
Alessandra
A
King
N Paul
NP
Shuker
Nicola
N
Steadman
Jon G A
JG
Takle
Andrew K
AK
Sanger
Gareth
G
Butler
Sharon
S
McKay
Fiona
F
Muir
Alison
A
Winborn
Kim
K
Ward
Robert W
RW
Heightman
Tom D
TD
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*
D054439:Ghrelin; D054440:Receptors, Ghrelin; D013450:Sulfones; D013006:Growth Hormone