結核菌に対する化学療法剤の研究(第18報) : Formyl-8-hydroxyquinoline誘導体の合成ならびに抗結核菌作用について

概要

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The three position isomers of 8-hydroxyquinolinecarboxaldehydes with the formyl group in 2-, 4-, or 5-position, and their derivatives, making a total of 42 compounds, were synthesized. The antibacterial activity of these compounds was tested against human-type tubercle bacilli H37Rv, sensitive strain, and the strain resistant to PAS, INAH, and streptomycin. It was thereby found that the introduction of a formyl group into 2- or 4-position of 8-hydroxyquinoline resulted in a marked decrease in a antibacterial action, while that in the 5-position showed no change from the original compound. The 2-substituted 8-hydroxyquinolinecarboxaldehyde thiosemicarbazones showed increased activity than the original formyl compound, but the 4-and 5-substituted derivatives showed rather a decrease in the activity. The antibacterial activity of 8-hydroxyquinoline-5-carboxaldehyde isonicotinoylhydrazone against the triple-resistant strain was much lower than that against the sensitive strain and this was assumed to be due to the presence of cross resistance with INAH, considering its structure.
社団法人日本薬学会の論文
1967-07-25