Studies on prodrugs. 5. Synthesis and antimicrobial activity of N-(oxoalkyl) norfloxacin derivatives

…, F Sakamoto, Y Kodera, G Tsukamoto

文献索引：Kondo, Hirosato; Sakamoto, Fumio; Kodera, Yasuo; Tsukamoto, Goro Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 2020 - 2024

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被引用次数: 40

摘要

Several N (oxoalky1) 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% ...