Publication

Synthesis and glycosidase inhibitory activity of 1-amino-3,6-anhydro-1-deoxy-D-sorbitol derivatives

Pierre Vogel, Claudia Bello
2010
Journal Articles

Résumé

3,6-Anhydro-1-(aryl or alkylamino)-1-deoxy-D-sorbitol derivatives have been prepared in four steps from isosorbide, a by-product from the starch industry. The inhibitory activities of these new compounds have been evaluated towards 13 glycosidases. A first lead-compound was identified, which inhibited beta-N-acetylglucosaminidase from bovine kidney (82% inhibition at 1 mM). (C) 2009 Elsevier Inc. All rights reserved.

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https://infoscience.epfl.ch/entities/publication/f0af1bd5-d446-49bc-bd22-80736d0b8749

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Pierre Vogel, Claudia Bello
2010
Journal Articles

Résumé

Source officielle

https://infoscience.epfl.ch/entities/publication/f0af1bd5-d446-49bc-bd22-80736d0b8749

À propos de ce résultat

Concepts associés (18)

Amidon

L'amidon (du latin amulum ou amylum, non moulu) est un glucide (sucre) complexe (polysaccharide ou polyoside) composé d'unités D-glucose (sucre simple). Il s'agit d'une molécule de réserve pour les végétaux supérieurs et un élément courant de l'alimentation humaine. Chez les animaux et les champignons, l'équivalent de l'amidon est le glycogène : molécule de stockage de glucides et donc d'énergie. L'amidon se trouve dans les organes de réserves de nombreuses plantes : les graines (en particulier la châtaigne, les céréales (blé, maïs, froment, etc.

Glucide

vignette|150px|Par exemple, le glucose est un glucide à six carbones, cinq groupes hydroxyle et un groupe aldéhyde. vignette|Les grains et céréales contiennent une grande quantité de glucides. Les glucides sont définis par l'Union internationale de chimie pure et appliquée (UICPA) comme une classe de composés organiques contenant un groupe carbonyle (aldéhyde ou cétone) et au moins deux groupes hydroxyle (-OH).

Corn starch

Corn starch, maize starch, or cornflour (British English) is the starch derived from corn (maize) grain. The starch is obtained from the endosperm of the kernel. Corn starch is a common food ingredient, often used to thicken sauces or soups, and to make corn syrup and other sugars. Corn starch is versatile, easily modified, and finds many uses in industry such as adhesives, in paper products, as an anti-sticking agent, and textile manufacturing. It has medical uses as well, such as to supply glucose for people with glycogen storage disease.

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Publications associées (14)

Generating macrocyclic inhibitors of protein-protein interactions

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Protein-protein interactions (PPIs) play important roles in many diseases and their modulation is an attractive strategy for developing new therapeutics. However, the relatively large and often flat binding surfaces of PPIs makes the development of inhibit ...

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The discovery of a drug requires over a decade of intensive research and financial investments – and still has a high risk of failure. To reduce this burden, we developed the NICEdrug.ch resource, which incorporates 250,000 bioactive molecules, and studied ...

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Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria

Paul Joseph Dyson, Thierry Laroche, John McKinney, Stewart Cole, Neeraj Dhar, Raphael Christopher Sommer, Joao Pedro De Almeida Neres, Raju Mukherjee, Jérémie Piton

Benzothiazinones (BTZ) are highly potent bactericidal inhibitors of mycobacteria and the lead compound, BTZ043, and the optimized drug candidate, PBTZ169, have potential for the treatment of tuberculosis. Here, we exploited the tractability of the BTZ scaf ...

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