Pyridone derivatives as potent and selective VLA-4 integrin antagonists

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2256-9. doi: 10.1016/j.bmcl.2006.01.025. Epub 2006 Feb 7.

Authors

Jason Witherington¹, Vincent Bordas, Alessandra Gaiba, Phil M Green, Antoinette Naylor, Nigel Parr, David G Smith, Andrew K Takle, Robert W Ward

Affiliation

¹ 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

PMID: 16455247
DOI: 10.1016/j.bmcl.2006.01.025

Abstract

A novel series of pyridone inhibitors has been identified through pharmacophore analysis, as potent antagonists of VLA-4.

MeSH terms

Binding Sites
Drug Design
Integrin alpha4beta1 / antagonists & inhibitors*
Pyridones / chemical synthesis*
Pyridones / pharmacology*
Structure-Activity Relationship
Vascular Cell Adhesion Molecule-1 / metabolism

Substances

Integrin alpha4beta1
Pyridones
Vascular Cell Adhesion Molecule-1