QUINOLONE DERIVATIVE OR ITS SALT AND ANTIMICROBIAL AGENT COMPRISING THE SAME

摘要

PURPOSE:To obtain a new compound as an antimicrobial agent having especially anti-HIV action and useful as a preventing and therapeutic agent for AIDS. CONSTITUTION:This compound is expressed by formula I [R is H or carboxy- protecting group; X is halogen; Y is halogen or cyclic amino; Z is H or halogen; A is formula II [R<2> to R<5> are H, lower alkyl, lower alkenyl or phenyl; (n) is 0, 2 or 3], e.g. ethyl 1-(aziridin-1-yl)-6,7-difluoro-1,4-dihydro-4-oxoquinoline-3- carboxylate. The compound expressed by formula I is obtained by reacting an amine expressed by formula III (Y<1> is halogen) with an olefin expressed by formula IV in the presence of lead tetraacetate in a solvent (e.g. benzene) at -40 to +50 deg.C. The compound expressed by formula I is capable of manifesting excellent antimicrobial activity against Gram-negative and Gram-positive bacteria, has high oral absorptivity and is useful as a medicine for human bodies and animals and further a medicine for fish diseases, an agrichemical and a preservative for foods.