As a new type of norfloxacin (NFLX) prodrug, N-(5-substituted 2-oxo-l, 3-dioxol-4-yl)methyl NFLXs were designed. These N-masked NFLXs were prepared and confirmed to produce higher NFLX levels in blood than NFLX itself after oral administration to mice. N-(5-Methyl-2-oxo-l,3-dioxol-4-yl)methyl NFLX was found to be smoothly hydrolyzed in mouse blood in vitro, and when administered orally, gave about 5-fold higher blood levels of NFLX than NFLX itself. Thus, the (5-methyl-2-oxo-l,3-dioxol-4-yl)methyl group was confirmed to function as an amine-type promoiety.
All Science Journal Classification (ASJC) codes
- Drug Discovery