A new fluoroquinolone derivative exhibits inhibitory activity against human immunodeficiency virus type 1 replication.
The inhibitory activity of several fluoroquinolone antibiotics against human immunodeficiency virus type 1 (HIV-1) replication was investigated. R-71762, (+/-) 9-fluoro-3-fluoromethyl-2, 3-dihydro-10-[4-(2-pyridyl)-1-piperazinyl]-7-oxo-7H-pyrido[1,2, 3-de][1,4]benzoxazine-6-carboxylic acid, protected MT-4 cells from HIV-1-induced cytopathic effects. Furthermore, the compound inhibited virus replication both in acutely and in chronically HIV-1-infected cells. On the other hand, ofloxacin, levofloxacin, ciprofloxacin, norfloxacin and enoxacin, that were previously reported to be protective against HIV-1-induced cytopathic effects, did not show any protective activity in our assay system. These results indicate that R-71762 is a novel inhibitor of HIV-1 replication and is effective even in HIV-1 chronically infected cells.
Kashiwase
H
H
Biological Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan. hiroto@shina.sankyo.co.jp
Momota
K
K
Ohmine
T
T
Komai
T
T
Kimura
T
T
Katsube
T
T
Nishigaki
T
T
Kimura
S
S
Shimada
K
K
Furukawa
H
H
D019380:Anti-HIV Agents / Q000494:pharmacology*; D000890:Anti-Infective Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D003588:Cytopathogenic Effect, Viral; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D064704:Levofloxacin; D008826:Microbial Sensitivity Tests; D015242:Ofloxacin / Q000031:analogs & derivatives* / Q000494:pharmacology; D014407:Tumor Cells, Cultured; D014779:Virus Replication / Q000187:drug effects*
D019380:Anti-HIV Agents; D000890:Anti-Infective Agents; C117133:R 71762; D064704:Levofloxacin; D015242:Ofloxacin