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Comparative Study
. 2002 Mar 11;12(5):739-42.
doi: 10.1016/s0960-894x(02)00003-3.

Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones

Toshinori Ohmine  1 , Tetsushi Katsube, Yasunori Tsuzaki, Miho Kazui, Nobuhiro Kobayashi, Tomoaki Komai, Masahiko Hagihara, Takashi Nishigaki, Aikichi Iwamoto, Tomio Kimura, Hiroto Kashiwase, Makoto Yamashita
Affiliations
Comparative Study

Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones

Toshinori Ohmine et al. Bioorg Med Chem Lett. .

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.

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