PURPOSE: To obtain a new compound having excellent antibacterial action and peroral absorbability and useful as an antibacterial agent.
CONSTITUTION: A compound of the formula I [R1 is H or carboxyl-protecting group; R2 is H, lower alkyl, lower alkoxy, hydroxyl, etc.; Y is halogen or saturated cyclic amino; X is N or -CR4= (R4 is H or halogen); R3 is thiazolyl], e.g. 6,7-difluoro-1-(thiazol-4-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid ethyl ester. The compound of the formula I can be produced by reacting a compound of the formula II (Y1 and Z are halogen; R1a is lower alkyl) with an orthoformic acid ester and a compound of the formula H2N-R3, cyclizing the obtained compound of the formula III and optionally hydrolyzing the product (when R1 is H or lower alkyl and Y is halogen). The compound of the formula I is useful as pharmaceutical agents for human and animal, agents for fish disease, agrochemicals and food preservatives. It is also expected to have antiviral action, especially anti-HIV action.
NODA HIDEICHIRO
MOCHIZUKI HARUYO
AMANO HIROTAKA
YAZAKI AKIRA
FUJISAWA PHARMACEUTICAL CO