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5-(3'-吲哚基)-2-硫代乙内酰脲衍生物作为醛糖还原酶抑制剂的合成及其构效关系研究

Studies on the synthesis and structure-activity relationships of 5-(3'-indolal)-2-thiohydantoin derivatives as aldose reductase enzyme inhibitors.

作者信息

Büyükbingöl E, Süzen S, Klopman G

机构信息

Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.

出版信息

Farmaco. 1994 Jun;49(6):443-7.

PMID:8074787
Abstract

A new series of 5-(3'-indolal)-2-thiohydantoin derivatives was synthesized and tested for the ability to inhibit bovine lens aldose reductase (AR) enzyme. The compounds were prepared by condensation of substituted indole-3-aldehyde derivatives with 2-thiohydantoin. The capacity of inhibiting the semi-purified bovine lens enzyme in vitro was observed for several of the compounds tested. One of them was found to be effective in reducing the enzyme activity compared with a corresponding well-known AR inhibitor.

摘要

合成了一系列新的5-(3'-吲哚醛基)-2-硫代乙内酰脲衍生物,并测试了它们抑制牛晶状体醛糖还原酶(AR)的能力。这些化合物通过取代吲哚-3-醛衍生物与2-硫代乙内酰脲缩合制备。在所测试的几种化合物中观察到了它们在体外抑制半纯化牛晶状体酶的能力。其中一种化合物与相应的知名AR抑制剂相比,被发现能有效降低酶活性。

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