| abstract |
Disclosed is a thioquinolone derivative which exhibits highly selective antibacterial activity against Helicobacter pylori and which is represented by the formula In n wherein R 1 and R 2 respectively represent hydrogen atom or R 1 and R 2 are joined to form ―O―(CH 2 ) 2 -; R 3 represents halogen atom, C 1 -C 12 alkyl group, C 1 -C 12 alkoxy group, lower alkylsulfonyloxy group, carboxy lower alkoxy group, lower alkylthio group, benzyloxy group, benzylthio group, phenoxy group, styryl group, nitro group, phenyl group, naphthyl group, piperazinyl group, morpholino group or hydroxyl group or represents ―CH 2 R 5 , ―COR 6 or ―NR 7 R 8 wherein R 5 represents benzyl group, phenyl group, hydroxyl group, lower alkoxy group, lower alkylcarbonyloxy group, phenoxy group, di-lower alkylamino group or benzimidazolylthio group, R 6 represents lower alkyl group or amino group and R 7 and R 8 respectively represent lower alkyl group; and R 4 represents hydrogen atom or lower alkyl group or is coupled with R 3 to form cyclohexene ring, benzene ring or pyridine ring, R 3 being not halogen atom at any of positions 5 to 8, methyl group at position 6 or methoxy group at position 6 of the quinoline ring when R 1 , R 2 and R 4 are respectively hydrogen atom, R 3 and R 4 being not at positions 6 and 7 or positions 6 and 8 of the quinoline ring when R 1 and R 2 are respectively hydrogen atom and R 4 is lower alkyl group. |