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Bioorg Med Chem Lett. 2010 Jan 15;20(2):594-9. doi: 10.1016/j.bmcl.2009.11.093. Epub 2009 Nov 22.

Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.

Author information

1
F. Hoffmann-La Roche Ltd, Discovery Research Basel, CH-4070 Basel, Switzerland. eric_a.kitas@roche.com

Abstract

Sulfonylureido thiazoles were identified from a HTS campaign and optimized through a combination of structure-activity studies, X-ray crystallography and molecular modeling to yield potent inhibitors of fructose-1,6-bisphosphatase. Compound 12 showed favorable ADME properties, for example, F=70%, and a robust 32% glucose reduction in the acute db/db mouse model for Type-2 diabetes.

PMID:
19969452
DOI:
10.1016/j.bmcl.2009.11.093
[Indexed for MEDLINE]

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