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Summary
Novelty: Novel quinoline, naphthyridine and pyridobezoxazine derivatives are disclosed. The compounds are potentially useful against microbial pathogens.
Biology: The antibacterial activity of the compounds is demonstrated against a wide variety of bacteria including Staphylococcus aureus, Micrococcus leuteus and Pseudomonas aeruginosa. Additionally, the in vivo antibacterial activity of a specific compound is determined by studying the protection of CF-1 female mice from bacterial challenge (Staphylococcus aureus). An oral ED50 of 6.0 mg/kg/day and a subcutaneous ED50 of 5.0mg/kg/day is obtained.
Chemistry: Thirty-three compounds are specifically claimed. Two of the specifically claimed compounds are 1-cyclopropyl-6,8-difluoro-7-(9-amino-1,4-dioxa-7-azaspiro [4,4]non-7-yl)-1,4-dihydro-4-oxo-3-quinoline-carboxylic acid and 7-(2-didimethylaminomethyl-1,4-dioxa-7-azaspiro[4.4]non-7-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,8-napthyridine-3-carboxylic acid. The preparation of 552 compounds is either directly or indirectly exemplified. The preparative process is not claimed.