YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
結核菌に対する化学療法剤の研究 (第13報)
Pyridinaldehyd-thiosemicarbazon系化合物の合成並びに抗菌作用について
藤川 福二郎平井 邦夫内藤 益一津久間 俊次
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1959 年 79 巻 10 号 p. 1231-1234

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In order to test antibacterial activity, 36 kinds of 4-alkyl- and 4-arylthiosemicarbazones of pyridinealdehyde were synthesized, 2-Pyridinealdehyde 4-substituted thiosemicarbazones were prepared by application of 4-alkyl- and 4-arylthiosemicarbazides to pyridinealdehyde, while 3- and 4-pyridinealdehyde 4-substituted thiosemicarbazones were prepared by starting from nicotinic acid hydrazide and isonicotinic acid hydrazide, deriving them to 1-nicotinyl-2-benzenesulfonylhydrazine and 1-isonicotinyl-2-benzenesulfonylhydrazine, and application of 4-alkyl- or 4-arylthiosemicarbazide without forming the free aldehyde. Antitubercular tests of these compounds against human-type tubercle bacilli, H37Rv strain, gave following results:
1) Introduction of aryl group into nitrogen in 4-position of the thiosemicarbazono group (=N-NH-CS-NH2) showed stronger action than introduction of alkyl group.
2) Antibacterial activity of the 4-aryl- and 4-alkylthiosemicarbazones of 2-pyridinealdehyde was stronger than that of the original thiosemicarbazone, while those of 3- and 4-pyridinealdehydes were weaker than that of the original thiosemicarbazones.

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