SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists

Bioorg Med Chem Lett. 2010 Jan 1;20(1):65-8. doi: 10.1016/j.bmcl.2009.11.030. Epub 2009 Nov 14.

Abstract

Recently, a new class of selective integrin alpha5beta1inhibitors consisting of a heterocyclic based scaffold was published. Herein the SAR and pharmacokinetic profiles of N-phenyl piperidine derivatives are described.

MeSH terms

  • Administration, Oral
  • Aminopyridines / chemical synthesis
  • Aminopyridines / chemistry*
  • Aminopyridines / pharmacokinetics
  • Animals
  • Dogs
  • Drug Design
  • Integrin alpha5beta1 / antagonists & inhibitors*
  • Integrin alpha5beta1 / metabolism
  • Male
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemical synthesis
  • Phenylalanine / chemistry
  • Phenylalanine / pharmacokinetics
  • Piperidines / chemical synthesis
  • Piperidines / chemistry*
  • Piperidines / pharmacokinetics
  • Rats
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Aminopyridines
  • Integrin alpha5beta1
  • Piperidines
  • Phenylalanine