Published January 25, 2019 | Version v1
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Discovery of a Potent α ‑ Galactosidase Inhibitor by in Situ Analysis of a Library of Pyrrolizidine − (Thio)urea Hybrid Molecules Generated via Click Chemistry

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Description

The parallel synthesis of a 26-membered-library of aromatic/aliphatic-(thio)urea-linked pyrrolizidines followed by in situ biological evaluation toward α -galactosidases has been carried out. The combination of the (thio)urea-forming click reaction and the in situ screening is pioneer in the search for glycosidase inhibitors and has allowed the discovery of a potent co ff ee bean α -galactosidase inhibitor (IC 50 = 0.37 μ M, K i = 0.12 μ M) that has also showed inhibition against human lysosomal α -galactosidase ( α -Gal A, IC 50 = 5.3 μ M, K i = 4.2 μ M).

Abstract

Ministerio de Economía y Competitividad (CTQ2016-77270-R)

Abstract

Junta de Andalucía (FQM-345)

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URL
https://idus.us.es/handle//11441/82051
URN
urn:oai:idus.us.es:11441/82051

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Origin repository
USE