Discovery of orally available integrin alpha5beta1 antagonists

Bioorg Med Chem Lett. 2010 Jan 1;20(1):380-2. doi: 10.1016/j.bmcl.2009.10.073. Epub 2009 Oct 28.

Abstract

Previous research within our laboratories identified the 3-hydroxypyrrolidine scaffold 1 as a new and selective integrin alpha5beta1 inhibitor class which was designed for local administration. Herein the discovery of new orally available integrin alpha5beta1 inhibitor scaffolds for potential systemic treatment is described.

MeSH terms

  • Administration, Oral
  • Animals
  • Drug Design
  • Half-Life
  • Integrin alpha5beta1 / antagonists & inhibitors*
  • Integrin alpha5beta1 / metabolism
  • Male
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / chemistry*
  • Pyrrolidines / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship

Substances

  • Integrin alpha5beta1
  • Pyrrolidines
  • pyrrolidine