Pyridone derivatives as potent and selective VLA-4 integrin antagonists.
A novel series of pyridone inhibitors has been identified through pharmacophore analysis, as potent antagonists of VLA-4.
Witherington
Jason
J
Department of Medicinal Chemistry, Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Research Limited, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK. Jason_Witherington@GSK.com
Bordas
Vincent
V
Gaiba
Alessandra
A
Green
Phil M
PM
Naylor
Antoinette
A
Parr
Nigel
N
Smith
David G
DG
Takle
Andrew K
AK
Ward
Robert W
RW
D001665:Binding Sites; D015195:Drug Design; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors*; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D019010:Vascular Cell Adhesion Molecule-1 / Q000378:metabolism
D039041:Integrin alpha4beta1; D011728:Pyridones; D019010:Vascular Cell Adhesion Molecule-1