The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Optimisation of a series of benzazepine sulfonamide hit compounds identified from high throughput screening led to the discovery of a new series of tractable, potent motilin receptor agonists.
Bailey
James M
JM
Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG12NY, UK. james.m.bailey@gsk.com
Scott
Jackie S
JS
Basilla
Jonathan B
JB
Bolton
Victoria J
VJ
Boyfield
Izzy
I
Evans
David G
DG
Fleury
Etienne
E
Heightman
Tom D
TD
Jarvie
Emma M
EM
Lawless
Kirk
K
Matthews
Kim L
KL
McKay
Fiona
F
Mok
Hindy
H
Muir
Alison
A
Orlek
Barry S
BS
Sanger
Gareth J
GJ
Stemp
Geoffrey
G
Stevens
Alexander J
AJ
Thompson
Mervyn
M
Ward
John
J
Vaidya
Kalindi
K
Westaway
Susan M
SM
D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D002626:Chemistry, Pharmaceutical; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D055808:Drug Discovery; D008956:Models, Chemical; D015394:Molecular Structure; D011964:Receptors, Gastrointestinal Hormone / Q000819:agonists*; D018013:Receptors, Neuropeptide / Q000819:agonists*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000494:pharmacology*; D013450:Sulfones / Q000494:pharmacology*
D011964:Receptors, Gastrointestinal Hormone; D018013:Receptors, Neuropeptide; D013449:Sulfonamides; D013450:Sulfones; C050802:motilin receptor