4-Oxo-4H- (1,3) thiazeto (3,2-a) quinoline-3-carboxylic acid derivatives, as well as pharmaceutical preparation with antibacterial activity.

摘要

Quinolinecarboxylic acid derivatives represented by the following general formula (I) and physiologically-acceptable salts thereof. CHEM wherein R1 is hydrogen, alkyl, or substituted or unsubstituted phenyl; R2 is hydrogen, alkyl, aikoxy, hydroxy, halogen, nitro or substituted or unsubstituted amino; R3 is hydrogen or optionally-substituted alkyl; R4 and R5 are same or different and are alkyl or hydroxyalkyl or R4 and R5 may be combined and may form a cyclic amino together with the adjacent nitrogen atom and said cyclic amino may also be substituted and may further contain nitrogen, oxygen or sulfur as hetero-atoms therein; and X is halogen. have been found to be very effective antibacterial therapeutic agents for systemic and local infectious diseases caused by P. aeruginosa and Grampositive and negative bacteria.