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 1a-c, and in vivo, they showed higher activity than that of compounds 1a-c. After oral administration of 3-formyl compounds 8a-c to mice, the compounds were rapidly metabolized into 3-carboxyl compounds 1a-c. In particular, the 3-formyl derivative (8a) of norfloxacin (NFLX, 1a) gave a 2-fold higher serum level than that of NFLX and functioned as a prodrug of NFLX.
Original language | English |
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Pages (from-to) | 221-225 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 31 |
Issue number | 1 |
DOIs | |
Publication status | Published - Jan 1 1988 |
Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery