Pyridonecarboxylic acids as antibacterial agents. VIII. Synthesis and structure-activity relationship of 7-(1-aminocyclopropyl)-4-oxo-1,8-naphthyridine-3-carboxylic acids and 7-(1-aminocyclopropyl)-4-oxoquinoline-3-carboxylic acids
| Autor: | Nagako Nishida, Yozo Todo, Yoshiko Yamashiro, Yoshikazu Fukuoka, Jun Nitta, Saikawa Isamu, Mikako Miyajima, Hirokazu Narita |
|---|---|
| Rok vydání: | 1994 |
| Předmět: |
Cell Survival
Gram-Positive Bacteria Medicinal chemistry Chemical synthesis Cell Line Mice Structure-Activity Relationship Anti-Infective Agents In vivo Seizures Cricetinae Drug Discovery Gram-Negative Bacteria medicine Structure–activity relationship Animals Antibacterial agent 4-Quinolones biology Chemistry Brain General Chemistry General Medicine biology.organism_classification Ciprofloxacin Ofloxacin Antibacterial activity Bacteria medicine.drug |
| Zdroj: | Chemicalpharmaceutical bulletin. 42(10) |
| ISSN: | 0009-2363 |
| Popis: | 4-Oxo-1, 8-naphthyridine- and 4-oxoquinoline-3-carboxylic acids (2a, b and 3a-l) possessing a 1-amino-cyclopropyl group at the 7-position have been synthesized and evaluated for in vitro antibacterial activities. The three quinolones (3d, h, i) exhibited potent antibacterial activities against both gram-positive and gram-negative bacteria, which are comparable to those of ciprofloxacin (CPFX) and ofloxacin (OFLX). Among the three compounds, the best pharmacological and pharmacokinetic profile was obtained with 3i, an OFLX analogue, which was considerably less toxic than three reference quinolones (1, CPFX, and OFLX). |
| Databáze: | OpenAIRE |
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