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新型三唑、四嗪、噻二唑的合成及其生物活性。

Synthesis of novel triazoles, tetrazine, thiadiazoles and their biological activities.

作者信息

Al-Omair Mohammed A, Sayed Abdelwahed R, Youssef Magdy M

机构信息

Department of Chemistry, Faculty of Science, King Faisal University, Hofuf 31982, Saudi Arabia.

Department of Chemistry, Faculty of Science, University of Beni Suef, Beni Suef 62511, Egypt.

出版信息

Molecules. 2015 Feb 2;20(2):2591-610. doi: 10.3390/molecules20022591.

Abstract

An expedient synthesis of novel triazoles, tetrazine and thiadiazoles, using conveniently accessible and commercially available starting materials has been achieved. The synthesized compounds were characterized by spectroscopic and elemental analyses, and screened for their antibacterial activities against four different strains, namely E. coli, P. aeruginosa, S. aureus and B. megaterium. In particular, the compounds 5, 24 and 26h exhibited excellent antibacterial activities compared to the reference antibiotic. To get further insight about their behavior, these compounds were tested for their antioxidant activities via SOD-like activity, DPPH free radical scavenging activity, ABST and NO, which showed promising results. Furthermore, these compounds effectively promoted the cleavage of genomic DNA as well, in the absence of any external additives.

摘要

利用方便可得且市售的起始原料,实现了新型三唑、四嗪和噻二唑的便捷合成。通过光谱和元素分析对合成的化合物进行了表征,并针对四种不同菌株,即大肠杆菌、铜绿假单胞菌、金黄色葡萄球菌和巨大芽孢杆菌,对其抗菌活性进行了筛选。特别是,与参考抗生素相比,化合物5、24和26h表现出优异的抗菌活性。为了进一步了解它们的行为,通过超氧化物歧化酶样活性、DPPH自由基清除活性、ABST和NO对这些化合物的抗氧化活性进行了测试,结果显示出良好的前景。此外,在没有任何外部添加剂的情况下,这些化合物也有效地促进了基因组DNA的裂解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c5b/6272378/ca37cbe4b1a1/molecules-20-02591-g005.jpg

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