title: Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
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.
authors.affiliation: Respiratory and Inflammation Research Area, AstraZeneca, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. john.cumming@astrzeneca.com
authors.forename: John G
authors.initials: JG
authors.lastname: Cumming
authors.forename: Simon J
authors.initials: SJ
authors.lastname: Brown
authors.forename: Anne E
authors.initials: AE
authors.lastname: Cooper
authors.forename: Alan W
authors.initials: AW
authors.lastname: Faull
authors.forename: Anthony P
authors.initials: AP
authors.lastname: Flynn
authors.forename: Ken
authors.initials: K
authors.lastname: Grime
authors.forename: John
authors.initials: J
authors.lastname: Oldfield
authors.forename: John S
authors.initials: JS
authors.lastname: Shaw
authors.forename: Emma
authors.initials: E
authors.lastname: Shepherd
authors.forename: Howard
authors.initials: H
authors.lastname: Tucker
authors.forename: David
authors.initials: D
authors.lastname: Whittaker
mesh_terms: D000083:Acetanilides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D000818:Animals; D065100:CCR5 Receptor Antagonists; D018360:Crystallography, X-Ray; D004285:Dogs; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000083:Acetanilides; D065100:CCR5 Receptor Antagonists; D010880:Piperidines; D013450:Sulfones