Pyridonecarboxylic Acids as Antibacterial Agents. I Synthesis and Structure-Activity Relationship of 1-Aryl-6-(4-dimethylaminophenyl)-4-pyridone-3-carboxylic Acids

A series of 1-aryl-6-(4-dimethylaminophenyl)-4-pyridone-3-carboxylic acids (7-33) has been prepared in order to evaluate antibacterial activity of N-aryl group within pyridonecarboxylic antibiotics. The in vitro minimum inhibitory concentration data as indicated in Table II, all compounds except fou...

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Published inYAKUGAKU ZASSHI Vol. 106; no. 9; pp. 775 - 781
Main Authors NARITA, HIROKAZU, KONISHI, YOSHINORI, NITTA, JUN, NAGAKI, HIDEYOSHI, KITAYAMA, ISAO, WATANABE, YASUO, SAIKAWA, ISAMU
Format Journal Article
LanguageJapanese
Published Japan The Pharmaceutical Society of Japan 01.09.1986
Subjects
antibacterial activity
antibiotic
Bacteria - drug effects
Drug Resistance, Microbial
Pyridones - chemical synthesis
Pyridones - pharmacology
ridone-3-carboxylic acid 1-aryl
Structure-Activity Relationship
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Summary:A series of 1-aryl-6-(4-dimethylaminophenyl)-4-pyridone-3-carboxylic acids (7-33) has been prepared in order to evaluate antibacterial activity of N-aryl group within pyridonecarboxylic antibiotics. The in vitro minimum inhibitory concentration data as indicated in Table II, all compounds except four compounds (18, 20, 21 and 29) exhibit considerably higher activity against gram-positive S. aureus than the parent N-ethyl compound 1 and nalidixic acid. Among the compounds having substituted 1-phenyl groups, 4'-hydroxy compound 9 and its 2'-fluoro and 2'-methyl derivatives (25 and 27) are significantly active against both gram-positive and negative bacteria.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ISSN:0031-6903
1347-5231
DOI:10.1248/yakushi1947.106.9_775