Studies on prodrugs. 5. Synthesis and antimicrobial activity of N-(oxoalkyl)norfloxacin derivatives.
Several N-(oxoalkyl)norfloxacin derivatives (3a-g) were synthesized and evaluated for antibacterial activity in vitro and in vivo. Most of the compounds exhibited in vitro activity comparable to that of norfloxacin for Gram-positive bacteria, whereas their activity was lower than for Gram-negative bacteria. N-(2-Oxopropyl)norfloxacin (3b) liberated norfloxacin in the blood after oral administration in mice, and the serum level of norfloxacin was about 3-fold higher than that of norfloxacin itself. Thus, 3b showed high antibacterial activity in vivo.
D000818:Animals; D001419:Bacteria / Q000187:drug effects; D001711:Biotransformation; D008297:Male; D051379:Mice; D009643:Norfloxacin / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology
D009643:Norfloxacin