Abstract
A series of α-glucosidase inhibitors with the oleanolic acid core and different cinnamic amide ligands were designed and synthesized. Their preliminary structure-activity relationships were analyzed. In general, the compounds with 3,28-disubstituted oleanolic acid exhibited stronger activity than those 28-monosubstituted analogues, and variation of cinnamic amide substitution significantly affected α-glucosidase inhibition activities. Most of the compounds showed potent inhibitory activity against α-glucosidase with much greater efficacy than a typical α-glucosidase inhibitor, acarbose.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amides / chemistry
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Amides / pharmacology
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Cinnamates / chemistry*
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Cinnamates / pharmacology*
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Diabetes Mellitus, Type 2 / drug therapy
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Glycoside Hydrolase Inhibitors*
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Humans
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / pharmacology
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Ligands
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Oleanolic Acid / chemistry*
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Oleanolic Acid / pharmacology*
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Structure-Activity Relationship
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alpha-Glucosidases / metabolism
Substances
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Amides
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Cinnamates
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Enzyme Inhibitors
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Glycoside Hydrolase Inhibitors
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Hypoglycemic Agents
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Ligands
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cinnamic acid
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Oleanolic Acid
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alpha-Glucosidases