Literature DB >> 11858992

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

Toshinori Ohmine1, Tetsushi Katsube, Yasunori Tsuzaki, Miho Kazui, Nobuhiro Kobayashi, Tomoaki Komai, Masahiko Hagihara, Takashi Nishigaki, Aikichi Iwamoto, Tomio Kimura, Hiroto Kashiwase, Makoto Yamashita.   

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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Year:  2002        PMID: 11858992     DOI: 10.1016/s0960-894x(02)00003-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Inhibition of human immunodeficiency virus type 1 tat-trans-activation-responsive region interaction by an antiviral quinolone derivative.

Authors:  Sara Richter; Cristina Parolin; Barbara Gatto; Claudia Del Vecchio; Egidio Brocca-Cofano; Arnaldo Fravolini; Giorgio Palù; Manlio Palumbo
Journal:  Antimicrob Agents Chemother       Date:  2004-05       Impact factor: 5.191

2.  New anti-human immunodeficiency virus type 1 6-aminoquinolones: mechanism of action.

Authors:  Cristina Parolin; Barbara Gatto; Claudia Del Vecchio; Teresa Pecere; Enzo Tramontano; Violetta Cecchetti; Arnaldo Fravolini; Sara Masiero; Manlio Palumbo; Giorgio Palù
Journal:  Antimicrob Agents Chemother       Date:  2003-03       Impact factor: 5.191

3.  Synthesis of difluoromethyl ethers with difluoromethyltriflate.

Authors:  Patrick S Fier; John F Hartwig
Journal:  Angew Chem Int Ed Engl       Date:  2013-01-10       Impact factor: 15.336

  3 in total

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