title: A potent and orally active HIV-1 integrase inhibitor.
abstract: A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. melissa_egbertson@merck.com
authors.forename: Melissa S
authors.initials: MS
authors.lastname: Egbertson
authors.forename: H Marie
authors.initials: HM
authors.lastname: Moritz
authors.forename: Jeffrey Y
authors.initials: JY
authors.lastname: Melamed
authors.forename: Wei
authors.initials: W
authors.lastname: Han
authors.forename: Debra S
authors.initials: DS
authors.lastname: Perlow
authors.forename: Michelle S
authors.initials: MS
authors.lastname: Kuo
authors.forename: Mark
authors.initials: M
authors.lastname: Embrey
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Vacca
authors.forename: Matthew M
authors.initials: MM
authors.lastname: Zrada
authors.forename: Amanda R
authors.initials: AR
authors.lastname: Cortes
authors.forename: Audrey
authors.initials: A
authors.lastname: Wallace
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Leonard
authors.forename: Daria J
authors.initials: DJ
authors.lastname: Hazuda
authors.forename: Michael D
authors.initials: MD
authors.lastname: Miller
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Felock
authors.forename: Kara A
authors.initials: KA
authors.lastname: Stillmock
authors.forename: Marc V
authors.initials: MV
authors.lastname: Witmer
authors.forename: William
authors.initials: W
authors.lastname: Schleif
authors.forename: Lori J
authors.initials: LJ
authors.lastname: Gabryelski
authors.forename: Gregory
authors.initials: G
authors.lastname: Moyer
authors.forename: Joan D
authors.initials: JD
authors.lastname: Ellis
authors.forename: Lixia
authors.initials: L
authors.lastname: Jin
authors.forename: Wei
authors.initials: W
authors.lastname: Xu
authors.forename: Matthew P
authors.initials: MP
authors.lastname: Braun
authors.forename: Kellem
authors.initials: K
authors.lastname: Kassahun
authors.forename: Nancy N
authors.initials: NN
authors.lastname: Tsou
authors.forename: Steven D
authors.initials: SD
authors.lastname: Young
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002478:Cells, Cultured; D019427:HIV Integrase / Q000187:drug effects / Q000235:genetics; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D009154:Mutation; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D019428:HIV Integrase Inhibitors; D009287:Naphthyridines; D019427:HIV Integrase