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N-[5-(3-吡啶基)-1,3,4-噻二唑-2-基]-N'-芳酰基脲的合成及其抗菌活性

[Synthesis and antimicrobial activity of N-[ 5-(3-pyridyl)-1, 3, 4-thiadiazol-2-yl] -N'-aroyl urea].

作者信息

Dong Xing-Gao, Yan Ling, Song Xin-Jian, Du Yin-Xiang

机构信息

Medical School, Hubei Institute for Nationalities, Enshi 445000, China.

出版信息

Yao Xue Xue Bao. 2007 Jan;42(1):108-10.

Abstract

To synthesize and evaluate antimicrobial activity of novel heterocyclic compounds, the corresponding title aroyl ureas have been synthesized by the reaction of 2-amino-5-(3-pyridyl)-1, 3, 4-thiadiazole with aroyl isocyanates. Their antimicrobial activities in vitro were tested by disk diffusion methods and broth microdilution according to M-27A protocol recommended by NCCLS. Twelve new compounds were obtained, and their structures were confirmed by MS, IR, 1H NMR and elemental analysis. The biological screening tests showed that most of the compounds have some antifungal activities in vitro. Aroyl ureas incorporating pyridyl thiadiazole ring may be developed as novel antifungal candidate drugs and are worthwhile to be further studied.

摘要

为了合成和评估新型杂环化合物的抗菌活性,通过2-氨基-5-(3-吡啶基)-1,3,4-噻二唑与芳酰基异氰酸酯的反应合成了相应的标题芳酰基脲。根据美国国家临床实验室标准委员会(NCCLS)推荐的M-27A方案,采用纸片扩散法和肉汤微量稀释法测试了它们的体外抗菌活性。得到了12个新化合物,其结构通过质谱(MS)、红外光谱(IR)、核磁共振氢谱(1H NMR)和元素分析得以确证。生物筛选试验表明,大多数化合物在体外具有一定的抗真菌活性。含有吡啶基噻二唑环的芳酰基脲有望开发成为新型抗真菌候选药物,值得进一步研究。

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