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新型单和双吲哚康醇衍生物的合成及其α/β-糖苷酶抑制作用。

Synthesis of novel mono and bis-indole conduritol derivatives and their α/β-glycosidase inhibitory effects.

机构信息

Dumlupınar University, Education Faculty, 43100 Kutahya, Turkey.

出版信息

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7499-503. doi: 10.1016/j.bmcl.2012.10.038. Epub 2012 Oct 23.

Abstract

Here we synthesized four novel indole conduritol derivatives 1-4 for the first time in the literature and probed their biological activities with the α and β-glucosidases. The compounds showed quite effective glucosidase inhibitory action. IC(50) values of the compounds were compared with the known glucosidase inhibitor acarbose and it was determined that newly synthesized indole conduritols had more powerful effect against β-glucosidase in addition to exhibiting moderate influence against α-glucosidase. Our molecules thus constitute an important starting point for the design and exploitation of novel glucosidase inhibitors since glucosidase inhibitors have widespread applications in the treatment of diabetes, viral infections, lysosomal storage diseases and cancers.

摘要

在这里,我们首次合成了四个新型吲哚古洛糖醇衍生物 1-4,并研究了它们与α和β-葡萄糖苷酶的生物活性。这些化合物表现出相当有效的葡萄糖苷酶抑制作用。化合物的 IC50 值与已知的葡萄糖苷酶抑制剂阿卡波糖进行了比较,结果表明新合成的吲哚古洛糖醇除了对α-葡萄糖苷酶表现出适度的影响外,对β-葡萄糖苷酶也具有更强的作用。因此,我们的分子为设计和开发新型葡萄糖苷酶抑制剂提供了一个重要的起点,因为葡萄糖苷酶抑制剂在治疗糖尿病、病毒感染、溶酶体贮积病和癌症等方面有广泛的应用。

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