Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5538-41. doi: 10.1016/j.bmcl.2006.08.044. Epub 2006 Aug 22.

Authors

Jason Witherington¹, Emma L Blaney, Vincent Bordas, Richard L Elliott, Alessandra Gaiba, Neil Garton, Philip M Green, Antoinette Naylor, David G Smith, David J Spalding, Andrew K Takle, Robert W Ward

Affiliation

¹ 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

PMID: 16931004
DOI: 10.1016/j.bmcl.2006.08.044

Abstract

A series of pyridone-N-benzyl-propanoic acids have been optimised to afford potent orally bioavailable VLA-4 antagonists.

MeSH terms

Administration, Oral
Animals
Integrin alpha4beta1 / antagonists & inhibitors*
Pyridones / administration & dosage
Pyridones / pharmacokinetics
Pyridones / pharmacology*
Rats

Substances

Integrin alpha4beta1
Pyridones