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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) - 糠酮:一系列具有抗微生物活性的抗炎和镇痛化合物

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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(3H)-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:理想的抗炎药应具有最小剂量的所需效果,具有最小副作用。与这些试剂相关的抗微生物剂动作将是较额外的优势,因为它们拓宽了化合物的光谱。在我们以前的研究中合成的抗炎和抗微生物活性与一些2(3H) - 糠酮的低溃疡性,促使我们研究异丁烯对其药理学曲线的影响。由于化合物3,9,13和14除了低溃疡性发病率之外,它们还具有抗炎和镇痛作用,因此选择对各种环氧酶酶的抑制作用进行调查。发现它们对COX-2酶更具选择性。将6.25μg/ ml的MIC用于对针对金黄色葡萄球菌,大肠杆菌,R. Oryza和P. Citrum的化合物3,13和14的MIC。该研究支持呋喃酮衍生物作为具有抗微生物活性的潜在抗炎剂的发展。

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