Quinolone Antibacterial Agents Substituted at the 7-Position with Spiroamines. Synthesis and Structure-Activity Relationships

Article abstract of DOI:10.1021/jm00170a035

A series of fluoroquinolone antibacterials having the 7-position (10-position of pyridobenzoxazines) substituted with 2,7-diazaspiro<4.4>nonane (4b), 1,7-diazaspiro<4.4>nonane (5a), or 2,8-diazaspiro<5.5>undecane (6b) was prepared, and their biological activities were compared with piperazine and pyrrolidine substituted analogues.Most exhibited potent Gram-positive and Gram-negative activity, especially when side chain 4b was N-alkylated.