Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
A series of small molecule orally bioavailable ghrelin receptor agonists have been identified through systematic optimisation of a high throughput screening hit.
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
Briggs
Michael A
MA
Collis
Katharine
K
Dean
David K
DK
Gaiba
Alessandra
A
King
N Paul
NP
Kraus
Helmut
H
Shuker
Nicola
N
Steadman
Jon G A
JG
Takle
Andrew K
AK
Sanger
Gareth
G
Wadsworth
Graham
G
Butler
Sharon
S
McKay
Fiona
F
Muir
Alison
A
Winborn
Kim
K
Heightman
Tom D
TD
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D005453:Fluorescence; D007211:Indoles / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D044302:Receptor, Serotonin, 5-HT1B / Q000378:metabolism; D054440:Receptors, Ghrelin / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology*
D007211:Indoles; D044302:Receptor, Serotonin, 5-HT1B; D054440:Receptors, Ghrelin; C529346:SB-791016; D013449:Sulfonamides