Synthesis and biological activity of 5-amino-and 5-hydroxyquinolones, and the overwhelming influence of the remote N1-substituent in determining the structure- …
A series of 5-amino-and 5-hydroxyquinolone antibacterials substituted at C7 with a select group of common piperazinyl and 3-aminopyrrolidinyl side chains was prepared. These 5- substituted derivatives were compared to the analogous 5-hydrogen compounds for antiinfective activity by using DNA gyrase inhibition, minimum inhibitory concentrations against a variety of bacteria, and in vivo efficacy in the mouse infection model. The ...
