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设计、合成及 1,2,3-三唑糖苷点击连接子的抗菌活性。

Design, Synthesis, and Antimicrobial Activities of 1,2,3-Triazole Glycoside Clickamers.

机构信息

Photochemistry Department, Chemical Industries Research Division, National Research Centre, 33 El Buhouth Street, P.O. Box 12622 Cairo, Egypt.

Chemistry Department, Faculty of Science and Arts in Qurayat, Jouf University, P.O. Box 77425 Skaka, Kingdom of Saudi Arabia.

出版信息

Molecules. 2020 Feb 12;25(4):790. doi: 10.3390/molecules25040790.

Abstract

Bacterial resistance remains a significant threat and a leading cause of death worldwide, despite massive attempts to control infections. In an effort to develop biologically active antibacterial and antifungal agents, six novel aryl-substituted-1,2,3-triazoles linked to carbohydrate units were synthesized through the Cu(I)-catalyzed azide-alkyne cycloaddition CuAAC of substituted-arylazides with a selection of alkyne-functionalized sugars. The chemical structures of the new derivatives were verified using different spectroscopic techniques. The novel clicked 1,2,3-triazoles were evaluated for in vitro antibacterial activity against Gram-positive and Gram-negative and the obtained results were compared with the activity of the reference antibiotic "Ampicillin". Likewise, in vitro antifungal activity of the new 1,2,3-triazoles was investigated against and using "Nystatin" as a reference drug. The results of the biological evaluation pointed out that was more susceptible to all of the tested compounds than other examined microbes. In addition, some tested compounds exhibited promising antifungal activity.

摘要

尽管全球范围内已经采取了大规模的措施来控制感染,但细菌耐药性仍然是一个严重的威胁和全球主要的死亡原因。为了开发具有生物活性的抗菌和抗真菌药物,通过取代的芳基叠氮化物与一系列炔基官能化糖的 Cu (I) 催化的叠氮化物-炔烃环加成反应 CuAAC,合成了六个新型芳基取代的 1,2,3-三唑连接到糖单元上。利用不同的光谱技术验证了新衍生物的化学结构。新型点击 1,2,3-三唑化合物的体外抗菌活性对革兰氏阳性菌和革兰氏阴性菌进行了评价,并将所得结果与参考抗生素“氨苄西林”的活性进行了比较。同样,新型 1,2,3-三唑化合物的体外抗真菌活性也针对 和 进行了研究,以“制霉菌素”作为参考药物。生物评价的结果指出, 比其他被检查的微生物对所有测试的化合物都更敏感。此外,一些测试的化合物表现出有希望的抗真菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e56/7071105/825ac29033cd/molecules-25-00790-g001.jpg

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