Studies on antibacterial agents. III. Synthesis and antibacterial activities of substituted 1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acids.
A series of substituted 4-oxoquinoline-3-carboxylic acids having a methyl group at the 8-position was prepared and tested for their antibacterial activity. 7-(trans-3-Amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-6- fluoro-8-methyl-4-oxoquinoline-3-carboxylic acid (21) exhibited highly potent antibacterial activity against both gram-positive and gram-negative bacteria, including Pseudomonas aeruginosa.
Miyamoto
H
H
2nd Tokushima Institute of New Drugs Research, Otsuka Pharmaceutical Co., Ltd., Japan.
Ueda
H
H
Otsuka
T
T
Aki
S
S
Tamaoka
H
H
Tominaga
M
M
Nakagawa
K
K
D000150:Acinetobacter / Q000187:drug effects; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003521:Cyclopropanes / Q000138:chemical synthesis / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects
D000900:Anti-Bacterial Agents; D003521:Cyclopropanes; D011758:Pyrroles; D011804:Quinolines; D015363:Quinolones; C067414:7-(3-amino-4-methyl-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-6-fluoro-8-methyl-4-oxoquinoline-3-carboxylic acid