4-QUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS

摘要

A novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids (I) useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections. where Z is wherein one endocyclic double bond may be present between any two consecutive ring positions or two alternating or nonalternating endocyclic double bonds may be present in the ring; wherein n, n min , n''', and n sec sec are each independently 0, 1, or 2; n sec is 0, 1, 2, or 3; y is 0 or 1; x is 0 or 1; A and B are each independently CH, CH2, NR7 wherein R7 is hydrogen or R7 is R8CO wherein R8 is alkyl of from one to ten carbon atoms, arylalkyl, aryl wherein the aryl or alkyl may be substituted by hydroxy, halogen, COOH, or CONHR9 wherein R9 is hydrogen or alkyl of from one to four carbon atoms and when A is NR7, B can be O or S or when B is NR7, A can be absent; (CR13R14)n''' wherein R13 and R14 are each independently hydrogen or lower alkyl; and E is hydrogen, alkyl, OR10 wherein R10 is hydrogen or alkyl, NR11R12 wherein R11 and R12 are each independently hydrogen, lower alkyl, cycloalkyl alkylaryl, alkylheteroaryl, alkanoyl, amidine, peptide urethane, or R11 and R12 when taken together with the nitrogen to which they are attached form a ring of from three to six carbon atoms or