結核菌に対する化学療法剤の研究 (第13報)

Abstract

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.