首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Stereoselective synthesis and glycosidase inhibitory activity of 3,4-dihydroxy-pyrrolidin-2-one, 3,4-dihydroxy-piperidin-2-one and 1,2-dihydroxy-pyrrolizidin-3-one.
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Stereoselective synthesis and glycosidase inhibitory activity of 3,4-dihydroxy-pyrrolidin-2-one, 3,4-dihydroxy-piperidin-2-one and 1,2-dihydroxy-pyrrolizidin-3-one.

机译:3,4-二羟基-吡咯烷-2-酮,3,4-二羟基-哌啶-2-酮和1,2-二羟基-吡咯嗪丁-3-酮的立体选择性合成和糖苷酶抑制活性。

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摘要

3,4-Dihydroxy-pyrrolidin-2-one, 3,4-dihydroxy-piperidin-2-one and 1,2-dihydroxy-pyrrolizidin-3-one have been synthesized, using a simple strategy based on the asymmetric dihydroxylation of vinylogous aminoesters and subsequent mild intramolecular cyclization. All these compounds show a partial inhibition of alpha-glucosidase, but were inactive towards other glycosidases.
机译:使用基于乙烯基的不对称二羟基化的简单策略,合成了3,4-二羟基-吡咯烷-2-酮,3,4-二羟基-哌啶-2-酮和1,2-二羟基-吡咯烷酮-3-酮氨基酯和随后的轻度分子内环化。所有这些化合物均显示出对α-葡萄糖苷酶的部分抑制作用,但对其他糖苷酶无活性。

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