NOVEL QUINOLONE DERIVATIVE

摘要

NEW MATERIAL:A compound shown by formula I [R<1> is cycloalkyl, alkyl, alkenyl, phenyl, aralkyl, etc.; R2 is H, SH or alkylthio; R<3> is OH, OR<12> (R<12> is carboxy-protecting group), NH3, etc.; R<4> is H, halogen, OH, alkoxy, alkyl, NH2, etc.; R<5> is halogen, OH or alkoxy : R<6>-R<11> is H, halogen, alkyl, aryl, aminoalkyl, etc.; m is O or 1; X is N or CY (Y is H, halogen, alkyl, etc.)]. EXAMPLE:7-(3-Pyrrolin-1-yl)-1-cycIopropyl-6,8-difluoro-1,4-dihydro-4-o xoquinoline-3- carboxylic acid. USE:An antibacterial agent having extremely strong antibacterial activity against not only Gram-positive bacteria but also Gram-positive bacteria. PREPARATION:A compound shown by formula II is condensed with a 3-pyrroline shown by formula III or a 1,2,5,6-tetrahydropyridine derivative and optionally hydrolyzed to give a compound shown by formula I.