title: [2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.
abstract: Several series of CCR5 antagonists have been discovered by derivatization at the N-terminal of the piperidine ring of the core template 2. Some derivatives exhibited potent inhibition against HIV-1infection. The pharmacokinetic properties of the lead compounds 11a, 14a, 15b, and 16b have been evaluated in vivo.
authors.affiliation: Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.
authors.forename: Maosheng
authors.initials: M
authors.lastname: Duan
authors.forename: Christopher
authors.initials: C
authors.lastname: Aquino
authors.forename: Robert
authors.initials: R
authors.lastname: Ferris
authors.forename: Wieslaw M
authors.initials: WM
authors.lastname: Kazmierski
authors.forename: Terry
authors.initials: T
authors.lastname: Kenakin
authors.forename: Cecilia
authors.initials: C
authors.lastname: Koble
authors.forename: Pat
authors.initials: P
authors.lastname: Wheelan
authors.forename: Chris
authors.initials: C
authors.lastname: Watson
authors.forename: Michael
authors.initials: M
authors.lastname: Youngman
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D065100:CCR5 Receptor Antagonists; D016466:CHO Cells; D002626:Chemistry, Pharmaceutical / Q000379:methods; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000378:metabolism; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D051381:Rats; D019713:Receptors, CCR5 / Q000737:chemistry
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D010880:Piperidines; D019713:Receptors, CCR5; C032727:piperidine