Abstract
A novel series of non-covalent, benzimidazole-based inhibitors of DPP-4 has been developed from a small fragment hit using structure-based drug design. A highly versatile synthetic route was created for the development of SAR, which led to the discovery of potent and selective inhibitors with excellent pharmaceutical properties.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Benzimidazoles / chemical synthesis
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Benzimidazoles / pharmacology*
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Crystallography, X-Ray
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Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis
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Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
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Drug Design*
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / pharmacology*
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Models, Chemical
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Rats
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Dipeptidyl-Peptidase IV Inhibitors
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Hypoglycemic Agents
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benzimidazole