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从长链脂肪酸合成一些新型 2,5-取代噻唑烷二酮作为潜在的抗炎、镇痛和清除过氧化氢的试剂。

Synthesis of some novel 2,5-disubstituted thiazolidinones from a long chain fatty acid as possible anti-inflammatory, analgesic and hydrogen peroxide scavenging agents.

机构信息

Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, India.

出版信息

J Enzyme Inhib Med Chem. 2011 Apr;26(2):198-203. doi: 10.3109/14756366.2010.489897. Epub 2010 Jun 28.

Abstract

Some new decanoic acid [2,5-disubstituted-4-oxo-thiazolidin-3-yl]amides (6a-j) have been synthesised by the condensation of decanoic acid hydrazide with various aromatic aldehydes to yield the Schiff's bases. Cyclocondensation of the Schiff's bases with thioglycollic acid afforded 4-thiazolidinone derivatives. The structures of the newly synthesised compounds were confirmed by analytical and spectral methods. The anti-inflammatory, analgesic and antioxidant activity of the title compounds were evaluated. Compound 6j exhibited 44.84 % inhibition of inflammation and was the most potent anti-inflammatory agent of the series whereas compound 6f demonstrated the most potent analgesic activity (69.82% inhibition of writhing) followed by compounds 6e and 6g. All the synthesised compounds exhibited a potent antioxidant activity.

摘要

一些新的癸酸[2,5-二取代-4-氧代-噻唑烷-3-基]酰胺(6a-j)已经通过癸酸酰肼与各种芳香醛的缩合反应合成,得到希夫碱。希夫碱与巯基乙酸环缩合得到 4-噻唑烷酮衍生物。新合成的化合物的结构通过分析和光谱方法得到证实。评价了标题化合物的抗炎、镇痛和抗氧化活性。化合物 6j 表现出 44.84%的抗炎抑制作用,是该系列中最有效的抗炎剂,而化合物 6f 表现出最有效的镇痛活性(扭体抑制 69.82%),其次是化合物 6e 和 6g。所有合成的化合物都表现出很强的抗氧化活性。

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