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Carbasugar Probes to Explore the Enzyme Binding Pocket at the Anomeric Position: Application to the Design of Golgi Mannosidase II Inhibitors

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Abstract:

A methodology is described for the highly efficient and divergent synthesis of pseudosugars which allows the stereoselective introduction of polar groups at either the α or the β pseudoanomeric positions. Using this method, a series of 3-deoxycarbasugar analogues of mannose bearing a pyridyl group are rationally designed, prepared and tested for inhibition of Golgi α-mannosidase II.

Keywords: Carbasugar; Golgi mannosidase II; molecular modelling; synthesis

Document Type: Research Article

Publication date: October 1, 2013

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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