Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists.
A series of pyridone-N-benzyl-propanoic acids have been optimised to afford potent orally bioavailable VLA-4 antagonists.
Witherington
Jason
J
Department of DMPK and Medicinal Chemistry, Neurology and 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
Blaney
Emma L
EL
Bordas
Vincent
V
Elliott
Richard L
RL
Gaiba
Alessandra
A
Garton
Neil
N
Green
Philip M
PM
Naylor
Antoinette
A
Smith
David G
DG
Spalding
David J
DJ
Takle
Andrew K
AK
Ward
Robert W
RW
D000284:Administration, Oral; D000818:Animals; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors*; D011728:Pyridones / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats
D039041:Integrin alpha4beta1; D011728:Pyridones