Studies on prodrugs. 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives

…, F Sakamoto, K Kawakami, G Tsukamoto

Index: Kondo; Sakamoto; Kawakami; Tsukamoto Journal of Medicinal Chemistry, 1988 , vol. 31, # 1 p. 221 - 225

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Citation Number: 38

Abstract

Several 3-formylquinolone derivatives (8a-c) were synthesized to assay the antibacterial activity both in vitro and in vivo. In vitro, all of the compounds 8a-c showed lower activity than that of the corresponding 3-carboxyl compounds la-c, and in vivo, they showed higher activity than that of compounds la-c. After oral administration of 3-formyl compounds 8a-c to mice, the compounds were rapidly metabolized into 3-carboxyl compounds la-c. In ...