Synthesis and anti-HIV activity of arylpiperazinyl fluoroquinolones: a new class of anti-HIV agents.
Synthesis and anti-HIV activity of a series of novel arylpiperazinyl fluoroquinolones are reported. In the SAR study, the aryl substituents on the piperazine nitrogen were found to play an important role for the anti-HIV-1 activity. A few of the compounds exhibited potent anti-HIV activity: IC50=0.06 microM in chronically infected cells.
Hagihara
M
M
Pharmaceutical Research Department, Ube Laboratory, Ube Industries, Ltd., Ube City, Yamaguchi, Japan.
Kashiwase
H
H
Katsube
T
T
Kimura
T
T
Komai
T
T
Momota
K
K
Ohmine
T
T
Nishigaki
T
T
Kimura
S
S
Shimada
K
K
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016655:HIV Core Protein p24 / Q000032:analysis; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D015242:Ofloxacin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014779:Virus Replication / Q000187:drug effects
D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; D016655:HIV Core Protein p24; C117133:R 71762; D015242:Ofloxacin