A new fluoroquinolone derivative exhibits inhibitory activity against human immunodeficiency virus type 1 replication

The inhibitory activity of several fluoroquinolone antibiotics against huma n immunodeficiency virus type 1 (HIV-1) replication was investigated. R-717 62, (+/-) 9-fluoro-3-fluoromethyl-2,3-dihydro-10-[4-(2-pyridyl)-1-piperazin yl] -7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acid, protected MT-4 cells from HIV-l-induced cytopathic effects. Furthermore, the compoun d inhibited virus replication both in acutely and in chronically HIV-l-infe cted cells. On the other hand, ofloxacin, levofloxacin, ciprofloxacin, norf loxacin and enoxacin, that were previously reported to be protective agains t HIV-l-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 c ells.