Studies on prodrugs. 11. Synthesis and antimicrobial activity of N-[(4-methyl-5-methylene-2-oxo-1, 3-dioxolan-4-yl) oxy] norfloxacin

H Kondo, F Sakamoto, T Uno, Y Kawahata…

Index: Kondo, Hirosato; Sakamoto, Fumio; Uno, Toshio; Kawahata, Yoshihiro; Tsukamoto, Goro Journal of Medicinal Chemistry, 1989 , vol. 32, # 3 p. 671 - 674

Full Text: HTML

Citation Number: 24

Abstract

N-[(4-methyl-5-methylene-2-oxo-1, 3-dioxolan-4-yl) oxy] norfloxacin (4). In vitro, 4 exhibited lower activity than that of norfloxacin (NFLX, 1) for both Gram-positive and Gram-negative bacteria. However, in vivo the activity of 4 was higher than that of NFLX. Bioavailability studies in mice showed that 4 liberated a higher concentration of NFLX in plasma than NFLX itself when administered orally. From these data, 4 obtained by the chemical oxidation of 2 ...