Pyridonecarboxylic Acids as Antibacterial Agents. VI. Synthesis and Structure-Activity Relationship of 7-(Alkyl, Cycloalkyl, and Vinyl)-1-cyclopropyl-6-fluoro-4-quinolone-3-carboxylic Acids
| Autor: | Hirokazu Narita, Yoshikazu Fukuoka, Saikawa Isamu, Hiroyasu Takag, Yozo Todo, Fumihiko Iino, Keiichi Tanaka, Yasushi Ikeda |
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| Rok vydání: | 1994 |
| Předmět: |
Male
medicine.drug_class Stereochemistry Gram-Positive Bacteria Medicinal chemistry Chemical synthesis Mice Structure-Activity Relationship Anti-Infective Agents Seizures Gram-Negative Bacteria Drug Discovery medicine Animals Structure–activity relationship Alkyl Antibacterial agent chemistry.chemical_classification Mice Inbred ICR 4-Quinolones biology Chemistry General Chemistry General Medicine biology.organism_classification Quinolone Ciprofloxacin Antibacterial activity Bacteria medicine.drug |
| Zdroj: | Chemical and Pharmaceutical Bulletin. 42:2049-2054 |
| ISSN: | 1347-5223 0009-2363 |
| DOI: | 10.1248/cpb.42.2049 |
| Popis: | The title compounds (1a-i) have been synthesized starting with ethyl 1-cyclopropyl-6, 7-difluoro-4-quinolone-3-carboxylate (2). The 7-cyclopropyl and 7-vinyl derivatives (1e and 1i) exhibited potent in vitro antibacterial activities against both gram-positive and gram-negative bacteria, being equipotent with ciprofloxacin (CPFX) except for the activity against Pseudomonas aeruginosa. The two compounds were significantly less toxic than CPFX in terms of convulsion-induction as determined by intracerebral administration to mice, but showed lower urinary recoveries on intravenous administration. |
| Databáze: | OpenAIRE |
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