合成化学療法薬(第5報)Thiazolo[5,4-f]quinolinecarboxylic Acid誘導体の抗菌活性

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Antimicrobial activities of 98 thiazoloquinolinecarboxylic acids were determined in vitro. Activities were classified into four groups, +++, ++, +, -, based on the average bacteriostatic index calculated by the equation, log_2 [100/MIC (μg/ml)]. In the 2,6-disubstituted derivatives, 2-alkoxy compounds were active only against Gram-positive bacteria, while 2-HO, MeO_2S and NC derivatives were active only against Gram-negative bacteria. 2-Amino and 2-carbamoyl compounds had no activities. In the 3,6-dialkyl-2-oxo derivatives, the most effective alkyl substituent was Me or Et group. Replacement of 2-oxo group by thioxo, imino or hydrazino group resulted in lowering of the activities. The maximum activity of 3-N-alkyl compounds existed in the Me group against both Gram-positive and -negative bacteria, while the corresponding 2-O-alkyl derivatives became stronger against Gram-positive bacteria, but weaker against Gram-negative bacteria with the increase in the length of methylene chain. 6-Ethyl-2,3,6,9-tetrahydro-3-methyl-2,9-dioxothiazolo [5,4-f] quinoline-8-carboxylic acid was found to have the highest activities against Gram-positive and -negative bacteria including Escherichia coli resistant to nalidixic acid and Pseudomonas aeruginosa.
公益社団法人日本薬学会の論文
1979-05-25