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