title: Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
abstract: A series of 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists containing a variety of fused heterocycles at the 4-position of the piperidine side chain has been discovered, which are orally bioavailable with potent anti-HIV activity.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, RY800-206, PO Box 2000, Rahway, NJ 07065, USA. dooseop_kim@merck.com <dooseop_kim@merck.com>
authors.forename: Dooseop
authors.initials: D
authors.lastname: Kim
authors.forename: Liping
authors.initials: L
authors.lastname: Wang
authors.forename: Jeffrey J
authors.initials: JJ
authors.lastname: Hale
authors.forename: Christopher L
authors.initials: CL
authors.lastname: Lynch
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Budhu
authors.forename: Malcolm
authors.initials: M
authors.lastname: Maccoss
authors.forename: Sander G
authors.initials: SG
authors.lastname: Mills
authors.forename: Lorraine
authors.initials: L
authors.lastname: Malkowitz
authors.forename: Sandra L
authors.initials: SL
authors.lastname: Gould
authors.forename: Julie A
authors.initials: JA
authors.lastname: DeMartino
authors.forename: Martin S
authors.initials: MS
authors.lastname: Springer
authors.forename: Daria
authors.initials: D
authors.lastname: Hazuda
authors.forename: Michael
authors.initials: M
authors.lastname: Miller
authors.forename: Joseph
authors.initials: J
authors.lastname: Kessler
authors.forename: Renee C
authors.initials: RC
authors.lastname: Hrin
authors.forename: Gwen
authors.initials: G
authors.lastname: Carver
authors.forename: Anthony
authors.initials: A
authors.lastname: Carella
authors.forename: Karen
authors.initials: K
authors.lastname: Henry
authors.forename: Janet
authors.initials: J
authors.lastname: Lineberger
authors.forename: William A
authors.initials: WA
authors.lastname: Schleif
authors.forename: Emilio A
authors.initials: EA
authors.lastname: Emini
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019380:Anti-HIV Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D065100:CCR5 Receptor Antagonists; D006367:HeLa Cells; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D011759:Pyrrolidines / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D019713:Receptors, CCR5 / Q000378:metabolism
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D006571:Heterocyclic Compounds; D011759:Pyrrolidines; D019713:Receptors, CCR5