新型香豆素衍生物的合成与评价及其作为抗氧化、抗菌和抗炎剂的活性。
Synthesis and Evaluation of New Coumarin Derivatives as Antioxidant, Antimicrobial, and Anti-Inflammatory Agents.
机构信息
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Medicinal Chemistry, National Research Centre, Cairo 12622, Egypt.
出版信息
Molecules. 2020 Jul 16;25(14):3251. doi: 10.3390/molecules25143251.
New pyranocoumarin and coumarin-sulfonamide derivatives were prepared and evaluated for their antioxidant, antimicrobial, and/or anti-inflammatory activities. Coumarin-sulfonamide compounds demonstrated significant antioxidant activity, while ,, ,, and , exhibited antimicrobial activity equal to or higher than the standard antimicrobials against at least one tested microorganism. Regarding the anti-inflammatory testing, pyranocoumarins , , and and coumarin-sulfonamide compound showed more potent antiproteinase activity than aspirin in vitro; however, five compounds were as potent as aspirin. The anti-inflammatory activity of the promising compounds was further assessed pharmacologically on formaldehyde-induced rat paw oedema and showed significant inhibition of oedema. For in vitro COX-inhibitory activity of coumarin derivatives, pyranocoumarin derivative was the most selective (SI = 152) and coumarin-sulfonamide derivative was most active toward COX-2 isozyme. The most active derivatives met the in silico criteria for orally active drugs; thus, they may serve as promising candidates to develop more potent and highly efficient antioxidant, antimicrobial, and/or anti-inflammatory agents.
新的吡喃并香豆素和香豆素-磺酰胺衍生物被制备并评估其抗氧化、抗菌和/或抗炎活性。香豆素-磺酰胺化合物表现出显著的抗氧化活性，而化合物 、 、 、 和 对至少一种测试的微生物具有与标准抗菌剂相当或更高的抗菌活性。关于抗炎测试，吡喃并香豆素 、 、 和香豆素-磺酰胺化合物 在体外显示出比阿司匹林更强的抗蛋白酶活性；然而，有五种化合物与阿司匹林一样有效。有前途的化合物的抗炎活性在甲醛诱导的大鼠足肿胀的药理学上进一步进行了评估，并显示出对肿胀的显著抑制作用。对于香豆素衍生物的体外 COX 抑制活性，吡喃并香豆素衍生物 是最具选择性的（SI = 152），而香豆素-磺酰胺衍生物 对 COX-2 同工酶最活跃。最活跃的衍生物符合口服活性药物的计算标准；因此，它们可能是开发更有效和高效的抗氧化、抗菌和/或抗炎剂的有前途的候选物。
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