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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >3-Arylidene-5-(4-isobutylphenyl)-2(3H)-furanones: a new series of anti-inflammatory and analgesic compounds having antimicrobial activity
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3-Arylidene-5-(4-isobutylphenyl)-2(3H)-furanones: a new series of anti-inflammatory and analgesic compounds having antimicrobial activity

机译:3-亚芳基-5-(4-异丁基苯基)-2(3H)-呋喃酮:具有抗菌活性的新系列抗炎和止痛化合物

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摘要

An ideal anti-inflammatory drug should have the desired effect in minimum dose with minimum side effects. Antimicrobial actions associated with such agents will be an added advantage as they broaden the spectrum of the compounds. Promising anti-inflammatory and antimicrobial activity together with low ulcerogenic properties of some 2(3 H )-furanones, synthesized in our previous study, prompted us to investigate the effect of the isobutyl group on their pharmacological profile. Since compounds 3 , 9 , 13 , and 14 have both anti-inflammatory and analgesic effects in addition to low ulcerogenic incidence, they were selected for investigation of their inhibitory effects on various cyclo-oxygenase enzymes. It was found that they were more selective toward COX-2 enzymes. An MIC of 6.25 μg/mL was recorded for compounds 3 , 13 , and 14 against S. aureus , E. coli , R. oryza , and P. citrum . The study supports the development of furanone derivatives as potential anti-inflammatory agents with antimicrobial activity.
机译:理想的抗炎药应以最小的剂量和最小的副作用达到所需的效果。与这类试剂相关的抗菌作用将是一个附加的优势,因为它们拓宽了化合物的范围。在我们先前的研究中合成的有希望的抗炎和抗菌活性以及一些2(3 H)-呋喃酮的低致溃疡性,促使我们研究异丁基对其药理作用的影响。由于化合物3,9,13和14除具有较低的致溃疡作用外,还具有抗炎和止痛作用,因此选择它们用于研究其对各种环加氧酶的抑制作用。发现它们对COX-2酶更具选择性。记录的化合物3,13和14对金黄色葡萄球菌,大肠杆菌,米曲霉和柑橘假单胞菌的MIC为6.25μg/ mL。该研究支持呋喃酮衍生物作为具有抗菌活性的潜在抗炎药的开发。

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