title: Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1.
abstract: We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model.
authors.affiliation: Department of Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. matthew.d.tallant@gsk.com
authors.forename: Matthew D
authors.initials: MD
authors.lastname: Tallant
authors.forename: Maosheng
authors.initials: M
authors.lastname: Duan
authors.forename: George A
authors.initials: GA
authors.lastname: Freeman
authors.forename: Robert G
authors.initials: RG
authors.lastname: Ferris
authors.forename: Mark P
authors.initials: MP
authors.lastname: Edelstein
authors.forename: Wieslaw M
authors.initials: WM
authors.lastname: Kazmierski
authors.forename: Pat J
authors.initials: PJ
authors.lastname: Wheelan
mesh_terms: D000818:Animals; D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D065100:CCR5 Receptor Antagonists; D002460:Cell Line; D004195:Disease Models, Animal; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects; D020128:Inhibitory Concentration 50; D011700:Putrescine / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D019380:Anti-HIV Agents; D065100:CCR5 Receptor Antagonists; D011700:Putrescine