title: Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones.
abstract: Anti-HIV-1 activities and pharmacokinetics of a series of novel arylpiperazinyl fluoroquinolones are reported. Modification at the C-8 position with a trifluoromethyl group was superior to that with a difluoromethoxy group to achieve higher anti-HIV-1 activity. Two compounds studied exhibited quite high anti-HIV-1 activities (IC(50)<50 nM) in vitro and high bioavailabilities (BA>90%) in monkeys.
authors.affiliation: Biological Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, 140-8710, Tokyo, Japan.
authors.forename: Toshinori
authors.initials: T
authors.lastname: Ohmine
authors.forename: Tetsushi
authors.initials: T
authors.lastname: Katsube
authors.forename: Yasunori
authors.initials: Y
authors.lastname: Tsuzaki
authors.forename: Miho
authors.initials: M
authors.lastname: Kazui
authors.forename: Nobuhiro
authors.initials: N
authors.lastname: Kobayashi
authors.forename: Tomoaki
authors.initials: T
authors.lastname: Komai
authors.forename: Masahiko
authors.initials: M
authors.lastname: Hagihara
authors.forename: Takashi
authors.initials: T
authors.lastname: Nishigaki
authors.forename: Aikichi
authors.initials: A
authors.lastname: Iwamoto
authors.forename: Tomio
authors.initials: T
authors.lastname: Kimura
authors.forename: Hiroto
authors.initials: H
authors.lastname: Kashiwase
authors.forename: Makoto
authors.initials: M
authors.lastname: Yamashita
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019380:Anti-HIV Agents / Q000493:pharmacokinetics* / Q000494:pharmacology*; D001682:Biological Availability; D005617:Chlorofluorocarbons, Methane / Q000737:chemistry; D024841:Fluoroquinolones / Q000493:pharmacokinetics* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects*; D008252:Macaca fascicularis; D015394:Molecular Structure; D051381:Rats; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D005617:Chlorofluorocarbons, Methane; D024841:Fluoroquinolones; C009554:fluoroform