Synthesis and Inhibitory Activity of Novel Aldose Inhibitor Reductase 1-Acetyl-1H-indole-3-acetate
李卓玲 1杨威龙 2赵珊 1王淑红 3李臣 2王志兵 1修志明2
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作者信息
1. 长春工业大学 化学与生命科学学院,吉林 长春 130012
2. 吉林医药学院 吉林省抗体工程科技协同创新中心,吉林 吉林 132013
3. 长春百纯和成医药科技有限公司,吉林 长春 130012
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摘要
醛糖还原酶抑制剂(ARIs)抑制多元醇途径的醛糖还原酶是治疗糖尿病并发症的重要策略.以 2-氯苯甲酸为起始原料,在碱性条件下经铜催化,与甘氨酸反应生成氯代邻羧基苯基甘氨酸,再与乙酸酐反应,生成N-乙酰基邻羧基苯甲酸.然后在吡啶催化下合环,生成1-乙酰基-1H-吲哚-3-乙酸酯(AIA),总收率为79.0%,纯度为99.0%.通过1 H NMR、13 C NMR和MS(ESI)对其结构进行表征,并对该化合物的的醛糖还原酶抑制活性进行测定,IC50 =9.4×10-2 μM.
Abstract
Inhibition of polyol pathway Aldose reductase by Aldose reductase inhibitors(ARIs)is an important strategy for the treatment of diabetic complications.In this experiment,2-chlorobenzoic acid was used as the starting material,under alkaline conditions,reacted with glycine to generate chloro-o-carboxyphenylglycine,and then reacted with acetic anhydride to generate N-acetyl-o-carboxybenzoic acid,and then pyridine catalyzed under the cyclone to form 1-acetyl-1H-indole-3-acetate(AIA).The total yield is 79.0%,and the purity is 99.0%.Its structure was characterized by 1 H NMR,13 C NMR and MS(ESI),and the aldose reductase inhibitory activity of the compound was determined,and its IC50 value was 9.4×10-2 μM.
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