Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra, 136119 India.
J Enzyme Inhib Med Chem. 2011 Aug;26(4):546-52. doi: 10.3109/14756366.2010.535796. Epub 2010 Dec 20.
Starting from capric acid, hydrazone and thiazolidin-4-one derivatives have been synthesized in the present investigation. Decanoic acid hydrazide was reacted appropriately to yield hydrazones, which were then cyclized to yield the corresponding thiazolidin-4-ones. The structures of the newly synthesized compounds were confirmed by analytical and spectral methods. Anti-inflammatory, analgesic, and hydrogen peroxide-scavenging activity of the title compounds were evaluated. Among synthesized compounds, 2-hydroxyphenyl thiazolidinone with 44.90% inhibition of inflammation was the most potent anti-inflammatory agent. Similarly, 4-methoxybenzylidine hydrazide with 64.90% inhibition of writhing was observed to be the most potent analgesic agent of the synthesized compounds. All the synthesized compounds exhibited potent hydrogen peroxide-scavenging activity.
本研究以辛酸为起始原料,合成了腙和噻唑烷-4-酮衍生物。癸酸酰肼经适当反应得到腙,然后环化得到相应的噻唑烷-4-酮。新合成化合物的结构通过分析和光谱方法得到确认。评价了标题化合物的抗炎、镇痛和清除过氧化氢活性。在所合成的化合物中,具有 44.90%炎症抑制作用的 2-羟基苯基噻唑烷酮是最有效的抗炎剂。同样,具有 64.90%扭体抑制作用的 4-甲氧基苯亚甲基腙是所合成化合物中最有效的镇痛剂。所有合成的化合物都表现出很强的清除过氧化氢的活性。