Naphthyridine antibacterial agents containing an α-amino acid in the side chain of the 7-substituent

Claim 1

A compound of the formula ##STR18## wherein X is N; Y is H, F, NH 2 , or OR 2 ; Z is ##STR19## R is H, alkyl of 1-6 carbon atoms or a cation; R 1 is alkyl of 1-6 carbon atoms, haloalkyl in which alkyl has 1-4 carbon atoms, vinyl, cycloalkyl of 3-6 carbon atoms, phenyl, naphthyl or phenyl or naphthyl substituted by halogen, hydroxy, amino or alkyl of 1-4 carbon atoms, indanyl, indolyl, quinolyl, isoquinolyl, 2-, 3-, or 4-pyridine, 2- or 3-thiophene, 2- or 3-furan, 2- or 4-imidazole, 2-oxazole or 2-thiazole; R 2 and R 3 are each independently hydrogen or alkyl of 1-4 carbon atoms; R 4 is --(CR 2 R 3 ) n --NR 2 R 5 in which n is 0, 1, or 2; R 5 is ##STR20## in which R 6 is hydrogen, alkyl of 1-10 carbon atoms, alkyl of 1-10 carbon atoms substituted by OR 2 , NR 2 R 3 , CO 2 H, CO 2 R 2 , CONR 2 R 3 , ##STR21## SR 2 , ##STR22## --CN, phenyl, naphthyl or phenyl or naphthyl substituted by halogen, hydroxy, amino, or alkyl of 1-4 carbon atoms, indanyl, indolyl, quinolyl, isoquinolyl, 2-, 3-, or 4-pyridine, 2- or 3-thiophene, 2- or 3-furan, 2- or 4-imidazole, 2-oxazole or 2-thiazole; or R 6 is phenyl, p-hydroxyphenyl or taken with the nitrogen atom of the α-amino group is trimethylene or hydroxy substituted trimethylene; and optically active isomer thereof, or a pharmaceutically acceptable acid addition salt thereof.