Synthesis and aldose reductase inhibitory activities of novel thienocinnolinone derivatives

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• 作者：Pau ; A. ; Asproni ; B. ; Boatto ; G. ; Grella ; G.E. ; De Caprariis ; P. ; Costantino ; L. ; Pinna ; G.A.
• 关键词：Diabetic complications ; Aldose reductase inhibitors ; Thieno[h]cinnolinone carboxylic acids
• 刊名：European Journal of Pharmaceutical Sciences
• 出版年：2004
• 出版时间：March, 2004
• 年：2004
• 卷：21
• 期：4
• 页码：545-552
• 全文大小：123 K

文摘

A novel series of tetrahydrothieno[2,3-h]cinnolinone derivatives were synthesized and evaluated in vitro for their ability to inhibit aldose reductase (ALR2), an enzyme involved in the appearance of diabetic complications. Compounds <b>2eb> and <b>2jb> exert a remarkable inhibitory effect, with ICb>50b> of 7.6 and 18μM, respectively. These compounds incorporate a valid pharmacophore for aldose reductase inhibitory activity represented by a thienocinnolinone template linked through a pentamethylene spacer to a carboxylic function.