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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2011-3-29
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pubmed:abstractText |
Inhibition of glycoside hydrolases has widespread application in treatment of diabetes, viral infections, lysosomal storage diseases and cancers. Gluco-configured tetrahydroimidazopyridines are the most potent ?-glucosidase inhibitors reported to date. Using transition state mimic strategy, a series of C2-substituted gluco-configured tetrahydroimidazopyridines were designed and synthesized. Compounds 3 (K(i)=0.64 nM) and 5 (K(i)=0.58 nM) showed stronger inhibitory potency against ?-glucosidase. Maestro 9.1 was used to study the structure-activity relationships by docking the compounds into the ?-glucosidase active sites.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3391
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pubmed:author |
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pubmed:copyrightInfo |
Crown Copyright © 2011. Published by Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2136-44
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pubmed:meshHeading |
pubmed-meshheading:21420868-Crystallography, X-Ray,
pubmed-meshheading:21420868-Enzyme Inhibitors,
pubmed-meshheading:21420868-Imidazoles,
pubmed-meshheading:21420868-Kinetics,
pubmed-meshheading:21420868-Models, Molecular,
pubmed-meshheading:21420868-Plant Extracts,
pubmed-meshheading:21420868-Prunus,
pubmed-meshheading:21420868-Pyridines,
pubmed-meshheading:21420868-Stereoisomerism,
pubmed-meshheading:21420868-Structure-Activity Relationship,
pubmed-meshheading:21420868-beta-Glucosidase
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pubmed:year |
2011
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pubmed:articleTitle |
Structure-activity relationships in a series of C2-substituted gluco-configured tetrahydroimidazopyridines as ?-glucosidase inhibitors.
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pubmed:affiliation |
College of Pharmacy, Nankai University, Tianjin 300071, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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