作者:JUNICHI HASE、KYOICHI KOBASHI、NOBUO KAWAGUCHI、KIYONORI SAKAMOTO
DOI:10.1248/cpb.19.363
日期:——
o-, m- and p-alkyloxybenzohydroxamic acids were synthesized and subjected to the examination for antibacterial and antifungal activity. All the hydroxamic acids tested were almost ineffective for pathogens examined of Enterobacteriaceae, but some of alkyloxybenzo- and fatty acyl-hydroxamic acid were found to be as highly effective for pathogenic fungi as butyl p-hydroxybenzoate being used as a comparison. The increase of carbon number of p-alkyloxybenzo- and fatty acyl-hydroxamic acid led to the increase in their antifungal activity, reached to the maximum at C6 in alkyloxy moiety and C10 in fatty acyl derivatives, and then the gradual decrease in both series. Considering the inhibitory power of hydroxamic acid on plant and bacterial urease, we discussed the possible correlation between antimicrobial activity and inhibitory powers on urease activity of the compounds.
o-、m- 和 p-烷氧基苯甲酰羟肟酸被合成并进行了抗菌和抗真菌活性的检测。所有测试的羟肟酸对所检测的肠杆菌科病原体几乎无效,但某些烷氧基苯甲酰和脂肪酸酰基羟肟酸被发现对病原真菌具有与作为比较标准的丁基对羟基苯甲酸酯相当的高效性。随着p-烷氧基苯甲酰和脂肪酸酰基羟肟酸中碳数的增加,其抗真菌活性也随之增强,在烷氧基部分达到C6和脂肪酸酰基衍生物部分达到C10时达到最高,随后在这两系列中逐渐下降。鉴于羟肟酸对植物和细菌脲酶的抑制作用,我们讨论了抗微生物活性与这些化合物对脲酶活性抑制能力之间可能的相关性。