title: Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
abstract: Cellular proliferation of HIV-1 requires the cooperative assistance of both the CCR5 and CD4 receptors. Our medicinal chemistry efforts in this area have resulted in the identification of N-alkyl piperidine sulfones as CCR5 antagonists. These compounds display potent binding and show antiviral properties in HIV-1 spread cell-based assays.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com
authors.forename: K
authors.initials: K
authors.lastname: Shankaran
authors.forename: Karla L
authors.initials: KL
authors.lastname: Donnelly
authors.forename: Shrenik K
authors.initials: SK
authors.lastname: Shah
authors.forename: Charles G
authors.initials: CG
authors.lastname: Caldwell
authors.forename: Ping
authors.initials: P
authors.lastname: Chen
authors.forename: Paul E
authors.initials: PE
authors.lastname: Finke
authors.forename: Bryan
authors.initials: B
authors.lastname: Oates
authors.forename: Malcolm
authors.initials: M
authors.lastname: MacCoss
authors.forename: Sander G
authors.initials: SG
authors.lastname: Mills
authors.forename: Julie A
authors.initials: JA
authors.lastname: DeMartino
authors.forename: Sandra L
authors.initials: SL
authors.lastname: Gould
authors.forename: Lorraine
authors.initials: L
authors.lastname: Malkowitz
authors.forename: Salvatore J
authors.initials: SJ
authors.lastname: Siciliano
authors.forename: Martin S
authors.initials: MS
authors.lastname: Springer
authors.forename: Gloria
authors.initials: G
authors.lastname: Kwei
authors.forename: Anthony
authors.initials: A
authors.lastname: Carella
authors.forename: Gwen
authors.initials: G
authors.lastname: Carver
authors.forename: Renee
authors.initials: R
authors.lastname: Danzeisen
authors.forename: Daria
authors.initials: D
authors.lastname: Hazuda
authors.forename: Karen
authors.initials: K
authors.lastname: Holmes
authors.forename: Joseph
authors.initials: J
authors.lastname: Kessler
authors.forename: Janet
authors.initials: J
authors.lastname: Lineberger
authors.forename: Michael D
authors.initials: MD
authors.lastname: Miller
authors.forename: Emilio A
authors.initials: EA
authors.lastname: Emini
authors.forename: William A
authors.initials: WA
authors.lastname: Schleif
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D065100:CCR5 Receptor Antagonists; D015704:CD4 Antigens / Q000378:metabolism; D002460:Cell Line; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D010880:Piperidines / Q000737:chemistry; D019713:Receptors, CCR5 / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D015704:CD4 Antigens; D010880:Piperidines; D019713:Receptors, CCR5; D013450:Sulfones; C032727:piperidine