Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides

  • Bioorg Med Chem Lett. 2006 Jul 1;16(13):3533-6. doi: 10.1016/j.bmcl.2006.03.089.
John G Cumming  1 ,  Simon J Brown ,  Anne E Cooper ,  Alan W Faull ,  Anthony P Flynn ,  Ken Grime ,  John Oldfield ,  John S Shaw ,  Emma Shepherd ,  Howard Tucker ,  David Whittaker
Affiliations
  • 1. Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. [email protected]
PMID: 16631366 DOI: 10.1016/j.bmcl.2006.03.089
Abstract

SAR and PK studies led to the identification of N-(1-{(3R)-3-(3,5-difluorophenyl)-3-[4-methanesulfonylphenyl] propyl}piperidin-4-yl)-N-ethyl-2-[4-methanesulfonylphenyl]acetamide as a highly potent and selective ligand for the human CCR5 Chemokine Receptor with good oral pharmacokinetic properties.