結核菌に対する化学療法剤の研究(第25報) : Azine系化合物およびp-Bromosalicyloylhydrazine誘導体の合成ならびに抗結核菌スクリーニングについて

概要

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Thirty kinds of azine series compounds and 29 kinds of p-bromosalicyloylhydrazine derivatives were synthesized and their antibacterial activity was tested against human tubercle bacilli, H37Rv strain. None of the azine series compounds proved to be effective when tested in the Kirchner medium added with 10% serum, using the sensitive strain and a strain resistant to three agents (>50 μg/ml of PAS, >50 μg/ml of INH, and>300μg/ml of streptomycin). Among the p-bromosalicyloylhydrazine derivatives tested in Tween-albumin medium, using a sensitive strain, p-bromosalicyloylhydrazones of 2-hydroxybenzaldehyde, 2-pyridinecarboxaldehyde, 2-hydroxy-1-naphthaldehyde, 8-hydroxy-5-quinolinecarboxaldehyde, and 8-hydroxy-2-quinolinecarboxaldehyde all inhibited bacillary growth at 12.5 μg/ml, indicating that the substitution of the amino group in p-aminosalicyloylhydrazine with bromine resulted in marked decrease of the antibacterial activity and that the presence of an amino group in the 4-position of PAS is a requisite for its antibacterial activity.
社団法人日本薬学会の論文
1970-01-25