Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 12, Issue 5, Pages 739-742Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(02)00003-3
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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. (C) 2002 Elsevier Science Ltd. All rights reserved.
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