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Bioorg Med Chem Lett. 2002 Mar 11;12(5):739-42.

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

Author information

  • 1Biological Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, 140-8710, Tokyo, Japan.

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.

PMID:
11858992
[PubMed - indexed for MEDLINE]
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