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N-桥连1-脱氧野尻霉素二聚体作为选择性昆虫海藻糖酶抑制剂。

N-Bridged 1-deoxynojirimycin dimers as selective insect trehalase inhibitors.

作者信息

Cipolla Laura, Sgambato Antonella, Forcella Matilde, Fusi Paola, Parenti Paolo, Cardona Francesca, Bini Davide

机构信息

Department of Biotechnology and Biosciences, University of Milano-Bicocca, Piazza della Scienza 2, 20126 Milano, Italy.

Department of Earth and Environmental Sciences, University of Milano-Bicocca, Piazza della Scienza 1, 20126 Milano, Italy.

出版信息

Carbohydr Res. 2014 May 7;389:46-9. doi: 10.1016/j.carres.2013.12.025. Epub 2014 Jan 30.

Abstract

A small set of N-bridged 1-deoxynojirimycin dimers has been synthesized and evaluated as potential inhibitors of insect trehalase from midge larvae of Chironomus riparius, porcine trehalase as the mammalian counterpart and α-amylase from human saliva. All the tested compounds (2-4) proved to be active (micromolar range activity) against insect trehalase, showing selectivity toward the insect glycosidase. No activity was observed against α-amylase.

摘要

已经合成了一小部分 N-桥连的 1-脱氧野尻霉素二聚体,并将其作为潜在抑制剂,用于评估其对摇蚊幼虫的昆虫海藻糖酶、作为哺乳动物对应物的猪海藻糖酶以及人唾液α-淀粉酶的抑制作用。所有测试化合物(2-4)均被证明对昆虫海藻糖酶具有活性(微摩尔范围活性),对昆虫糖苷酶表现出选择性。未观察到对α-淀粉酶的活性。

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