Author/Authors :
Toshinori Ohmine، نويسنده , , Tetsushi Katsube، نويسنده , , Yasunori Tsuzaki، نويسنده , , Miho Kazui، نويسنده , , Nobuhiro Kobayashi، نويسنده , , Tomoaki Komai، نويسنده , , Masahiko Hagihara، نويسنده , , Takashi Nishigaki، نويسنده , , Aikichi Iwamoto، نويسنده , , Tomio Kimura، نويسنده , , Hiroto Kashiwase، نويسنده , , Makoto Yamashita، نويسنده ,
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 (IC50<50 nM) in vitro and high bioavailabilities (BA>90%) in monkeys.
