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Bioorg Med Chem. 2011 Apr 1;19(7):2136-44. doi: 10.1016/j.bmc.2011.02.043. Epub 2011 Feb 26.

Structure-activity relationships in a series of C2-substituted gluco-configured tetrahydroimidazopyridines as β-glucosidase inhibitors.

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1
College of Pharmacy, Nankai University, Tianjin 300071, PR China.

Abstract

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 β-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 β-glucosidase. Maestro 9.1 was used to study the structure-activity relationships by docking the compounds into the β-glucosidase active sites.

PMID:
21420868
DOI:
10.1016/j.bmc.2011.02.043
[Indexed for MEDLINE]

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