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1,2,3-三唑噻唑杂合体的合成、体外抗菌活性和抗生物膜研究。

1,2,3-triazole-thiazole hybrids: Synthesis, in vitro antimicrobial activity and antibiofilm studies.

机构信息

Department of Chemistry, National Institute of Technology, Warangal 506004, Telangana, India; Environmental Monitoring &Exposure Assessment (Air) Laboratory, ICMR-NIREH, Bhopal 462 030, MP, India.

Medicinal Chemistry and Pharmacology Division, CSIR-IICT, Hyderabad 500 007, Telangana, India.

出版信息

Bioorg Med Chem Lett. 2021 Feb 1;33:127746. doi: 10.1016/j.bmcl.2020.127746. Epub 2020 Dec 15.

Abstract

A new series of triazole-thiazole hybrids were designed, synthesized by the Multi-component reaction approach and evaluated in vitro antimicrobial activity. Most of the tested series of compounds exhibited promising inhibitory activity against the bacterial strains with values in the range of 2.8 to 15.7 µM. The compounds 8i-8l and 8r showed potential-Candida activity against various Candida strains with spectrum values in the range 5.9-14.2 µM. Further, anti-biofilm and toxicity profiles for the potent compounds were also tested, and it was observed that the compounds 8i, 8k, and 8l were found to inhibit the biofilm formation with IC values of 6.6, 16.6 and 15.9 µM, respectively against Bacillus subtilis MTCC 121. Besides, 8k and 8l also displayed promising biofilm formation inhibitory activity towards Staphylococcus aureus MTCC 96 with IC values of 13.5 and 12.0 µM respectively. In summary, the activity results has emphasized the compounds 8k and 8l as potential leads for further development of antibacterial, anti-Candida, and anti-biofilm agents.

摘要

设计并通过多组分反应方法合成了一系列新的三唑噻唑杂合体,评估了它们的体外抗菌活性。大多数测试的化合物系列对细菌菌株具有有希望的抑制活性,其值在 2.8 到 15.7µM 之间。化合物 8i-8l 和 8r 对各种念珠菌菌株具有潜在的抗真菌活性,谱值在 5.9-14.2µM 之间。此外,还测试了潜在化合物的抗生物膜和毒性特征,结果表明化合物 8i、8k 和 8l 分别对枯草芽孢杆菌 MTCC 121 的生物膜形成具有抑制作用,IC 值为 6.6、16.6 和 15.9µM。此外,化合物 8k 和 8l 对金黄色葡萄球菌 MTCC 96 的生物膜形成也表现出有希望的抑制活性,IC 值分别为 13.5 和 12.0µM。总的来说,活性结果强调了化合物 8k 和 8l 作为进一步开发抗菌、抗真菌和抗生物膜剂的潜在先导化合物。

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