title: Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1.
abstract: Synthesis of several novel imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV are described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity and pharmacokinetics are highlighted. Several compounds with low nanomolar anti-HIV activity and oral bioavailability are described.
authors.affiliation: Department of Medicinal Chemistry, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. ksgudmundsson@gmail.com
authors.forename: Kristjan S
authors.initials: KS
authors.lastname: Gudmundsson
authors.forename: Sharon D
authors.initials: SD
authors.lastname: Boggs
authors.forename: John G
authors.initials: JG
authors.lastname: Catalano
authors.forename: Angilique
authors.initials: A
authors.lastname: Svolto
authors.forename: Andrew
authors.initials: A
authors.lastname: Spaltenstein
authors.forename: Michael
authors.initials: M
authors.lastname: Thomson
authors.forename: Pat
authors.initials: P
authors.lastname: Wheelan
authors.forename: Stephen
authors.initials: S
authors.lastname: Jenkinson
mesh_terms: D019380:Anti-HIV Agents / Q000493:pharmacokinetics / Q000627:therapeutic use; D000998:Antiviral Agents / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D006678:HIV / Q000737:chemistry; D015658:HIV Infections / Q000188:drug therapy; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008956:Models, Chemical
chemical_list: D019380:Anti-HIV Agents; D000998:Antiviral Agents