Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides

John G Cumming; Anne E Cooper; Ken Grime; Chris J Logan; Sharon McLaughlin; John Oldfield; John S Shaw; Howard Tucker; Jon Winter; David Whittaker

doi:10.1016/j.bmcl.2005.08.014

Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5012-5. doi: 10.1016/j.bmcl.2005.08.014.

Authors

John G Cumming¹, Anne E Cooper, Ken Grime, Chris J Logan, Sharon McLaughlin, John Oldfield, John S Shaw, Howard Tucker, Jon Winter, David Whittaker

Affiliation

¹ Respiratory & Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. john.cumming@astrazeneca.com

PMID: 16154744
DOI: 10.1016/j.bmcl.2005.08.014

Abstract

SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5 chemokine receptor.

MeSH terms

Animals
Benzeneacetamides / chemical synthesis
Benzeneacetamides / chemistry*
Benzeneacetamides / pharmacokinetics
Benzeneacetamides / pharmacology*
Biological Availability
CCR5 Receptor Antagonists*
Humans
Inhibitory Concentration 50
Ligands
Molecular Structure
Piperidines / chemistry*
Rats
Receptors, CCR5 / metabolism*
Structure-Activity Relationship

Substances

Benzeneacetamides
CCR5 Receptor Antagonists
Ligands
Piperidines
Receptors, CCR5
piperidine