結核化学療法の研究 (第11報)

2-Alkoxy-4-aminobenzoic Acidおよび4-Alkylaminosalicylic Acidの合成並びにその結核菌に対する抗菌作用

抄録

Some of 2-alkoxy-4-aminobenzoic acid, 4-alkylaminosalicylic acid, and 2-alkoxy-4-nitrobenzoic acid (alkyl=methyl, butyl, octyl, dodecyl, hexadecyl) were prepared and their bacteriostatic action against tubercle bacilli (human type) was tested in Kirchner medium. In these three compound series, it was found, as in other alkyl compounds already reported, that antibacterial activity increased with the number of carbon atoms in the alkyl, reached the maximum at around C₁₂, and decreased again over that number. The dodecyl derivatives of not only PAS but also of 4-nitrosalicylic acid, which by itself showed no remarkable activity, were as strongly antituberculous as PAS. This fact seems to suggest that, in some cases, even non-active compound may aquire strong antitubercular activity by introduction of alkyl group into it. The order of activity was: 4-alkylaminosalicylic acid>2-alkoxy-4-aminobenzoic acid>2-alkoxy-4-nitrobenzoic acid.