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新型酰腙衍生物的合成与抑菌活性研究。

Synthesis and antifungal activity of new hydrazide derivatives.

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University , Eskişehir , Turkey.

出版信息

J Enzyme Inhib Med Chem. 2013 Dec;28(6):1211-6. doi: 10.3109/14756366.2012.723208. Epub 2012 Sep 26.

Abstract

In this study, nine new hydrazide derivatives were synthesized. The reaction of 2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide with various benzaldehydes or acetophenones resulted in N'-substituted-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide derivatives. The structure elucidation of the synthesized and purified compounds was performed by using IR, (1)H-NMR, and FAB(+)-MS spectral data and elemental analyses, respectively. Furthermore, the compounds were screened and evaluated for their antifungal activity against a panel of different human pathogenic Candida strains such as C. albicans, C. glabrata, C. utilis, C. tropicalis, C. krusei, C. zeylanoides and C. parapsilosis using agar diffusion and broth microdilution assays, respectively. Some of the tested compounds showed comparable antifungal activity (MIC = 0.0156->2 mg/mL) with ketoconazole.

摘要

在这项研究中,合成了九个新的酰腙衍生物。2-[(5,6,7,8-四氢萘-2-基)氧基]乙二酰肼与各种苯甲醛或苯乙酮反应生成 N'-取代的 2-[(5,6,7,8-四氢萘-2-基)氧基]乙二酰肼衍生物。通过使用 IR、(1)H-NMR 和 FAB(+)-MS 光谱数据以及元素分析,分别对合成和纯化的化合物进行了结构阐明。此外,还使用琼脂扩散和肉汤微量稀释法分别对化合物进行了抗真菌活性筛选和评估,针对不同的人源致病性念珠菌菌株,如白色念珠菌、光滑念珠菌、近平滑念珠菌、热带念珠菌、克柔念珠菌、玉米赤霉和近平滑假丝酵母。一些测试的化合物显示出与酮康唑相当的抗真菌活性(MIC=0.0156->2mg/mL)。

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