Kutateladze Institute of Pharmacochemistry, Tbilisi State Medical University, Tbilisi, Georgia.
School of Pharmacy, Aristotle University, Thessaloniki, Greece.
SAR QSAR Environ Res. 2022 Apr;33(4):307-321. doi: 10.1080/1062936X.2022.2066173.
Herein we report the evaluation of the antimicrobial activity of some previously synthesized 3-(3,4-dihydroxyphenyl)glyceric acid in benzylated and in free 3,4 hydroxy groups in catechol moiety along with some caffeic and 3-(3,4-dihydroxyphenyl)glyceric acid amides using the microdilution method. The evaluation revealed that compounds showed in general moderate to low activity with MIC in range of 0.36-4.5 mg/mL. Compounds were also studied against three resistant bacteria strains MRSA (Methicillin-resistant and . Seven out of ten compounds were more potent than reference drugs ampicillin and streptomycin against MRSA, while against another two resistant strains seven compounds showed low activity and the rest were inactive. Antifungal activity of the tested compounds was much better than antibacterial, with MIC in the range of 0.019-3.0 mg/mL. Compounds #7 and 15 showed good activity against all fungi tested, being more potent than ketoconazole and in some case even better than bifonazole used as reference drugs. Docking studies revealed that the most active compound #7 binds to the haem group of the enzyme in the same way as ketoconazole.
在此，我们报告了一些先前合成的 3-(3,4-二羟基苯基)甘油酸在苄基化和儿茶酚部分的 3,4-羟基自由状态下的抗菌活性评估，以及一些咖啡酸和 3-(3,4-二羟基苯基)甘油酸酰胺的抗菌活性评估，采用微量稀释法。评估结果表明，化合物通常具有中等至低活性，MIC 范围为 0.36-4.5mg/mL。这些化合物还针对三种耐药菌 MRSA（耐甲氧西林金黄色葡萄球菌）、 和 进行了研究。十种化合物中有七种比参考药物氨苄西林和链霉素对 MRSA 更有效，而另外两种耐药菌株的七种化合物活性较低，其余的则无活性。与抗菌活性相比，测试化合物的抗真菌活性要好得多，MIC 范围为 0.019-3.0mg/mL。化合物 #7 和 15 对所有测试的真菌均表现出良好的活性，比酮康唑更有效，在某些情况下甚至比作为参考药物的比佛拉唑更好。对接研究表明，最有效的化合物 #7 以与酮康唑相同的方式与酶的血红素基团结合。
