含1,2,4-三唑、1,3,4-噻二唑和碳硫酰胺的新型吲哚衍生物的抗菌活性
Antimicrobial Activities of New Indole Derivatives Containing 1,2,4-Triazole, 1,3,4-Thiadiazole and Carbothioamide.
作者信息
Shirinzadeh Hanif, Süzen Sibel, Altanlar Nurten, Westwell Andrew D
机构信息
Erzincan University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Erzincan, Turkey.
Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
出版信息
Turk J Pharm Sci. 2018 Dec;15(3):291-297. doi: 10.4274/tjps.55707. Epub 2018 Nov 20.
OBJECTIVES
In new antimicrobial drug development studies, indole and its derivatives create an important class of compounds. In addition, azoles and their derivatives were recognized to be associated with a variety of biologic activities such as antibacterial and antifungal. In this study antimicrobial activities of some indole derivatives mainly substituted with 1,2,4-triazole, 1,3,4-thiadiazole and hydrazinecarbothioamide were investigated to evaluate their efficacy.
MATERIALS AND METHODS
The efficacy of new compounds was evaluated using 2-fold serial dilutions against , MRSA, , and .
RESULTS
The MIC was determined for test compounds and for the reference standards sultamicillin, ampicillin, fluconazole, and ciprofloxacin.
CONCLUSION
The compounds possessed a broad spectrum of activity having MIC values of 3.125-50 µg/mL against the tested microorganisms. This study provides valuable evidence that the indole-triazole derivative compound 3d holds significant promise as a novel antibacterial and antifungal lead compound.
目的
在新型抗菌药物研发研究中，吲哚及其衍生物构成了一类重要的化合物。此外，唑类及其衍生物被认为具有多种生物活性，如抗菌和抗真菌活性。在本研究中，对一些主要被1,2,4 - 三唑、1,3,4 - 噻二唑和肼基甲硫酰胺取代的吲哚衍生物的抗菌活性进行了研究，以评估它们的疗效。
材料与方法
使用2倍系列稀释法针对耐甲氧西林金黄色葡萄球菌（MRSA）、[此处原文缺失两种细菌名称]评估新化合物的疗效。
结果
测定了测试化合物以及参考标准药物舒他西林、氨苄西林、氟康唑和环丙沙星的最低抑菌浓度（MIC）。
结论
这些化合物具有广谱活性，对测试微生物的MIC值为3.125 - 50μg/mL。本研究提供了有价值的证据，表明吲哚 - 三唑衍生物化合物3d作为一种新型抗菌和抗真菌先导化合物具有巨大潜力。
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