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源自1-脱氧野尻霉素的双环异脲是β-葡萄糖脑苷脂酶的有效抑制剂。

Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase.

作者信息

Sevšek Alen, Čelan Maša, Erjavec Bibi, Quarles van Ufford Linda, Sastre Toraño Javier, Moret Ed E, Pieters Roland J, Martin Nathaniel I

机构信息

Utrecht Institute for Pharmaceutical Sciences, Utrecht University, Universiteitsweg 99, 3584 CG Utrecht, The Netherlands.

出版信息

Org Biomol Chem. 2016 Oct 7;14(37):8670-3. doi: 10.1039/c6ob01735e. Epub 2016 Sep 6.

DOI:10.1039/c6ob01735e
PMID:27604065
Abstract

A series of bicyclic isourea derivatives were prepared from 1-deoxynojirimycin using a concise synthetic protocol proceeding via a guanidino intermediate. Inhibition assays with a panel of glycosidases revealed that these deoxynojirimycin-derived bicyclic isoureas display very potent inhibition against human recombinant β-glucocerebrosidase with IC50 values in the low nanomolar range.

摘要

使用一种通过胍基中间体的简洁合成方案，从1-脱氧野尻霉素制备了一系列双环异脲衍生物。对一组糖苷酶的抑制试验表明，这些源自1-脱氧野尻霉素的双环异脲对人重组β-葡萄糖脑苷脂酶显示出非常有效的抑制作用，IC50值在低纳摩尔范围内。

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