Abstract
A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile.
MeSH terms
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Administration, Oral
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Aminobutyrates / chemical synthesis
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Aminobutyrates / chemistry*
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Aminobutyrates / pharmacokinetics
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Animals
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Caco-2 Cells
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Cell Line, Tumor
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Dipeptidyl Peptidase 4 / metabolism
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Dipeptidyl-Peptidase IV Inhibitors*
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Dogs
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Humans
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Hydrocarbons, Fluorinated / chemical synthesis
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Hydrocarbons, Fluorinated / chemistry*
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Hydrocarbons, Fluorinated / pharmacology
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / chemistry*
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Hypoglycemic Agents / pharmacokinetics
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Protease Inhibitors / chemical synthesis
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacokinetics
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Pyrrolidines / chemical synthesis
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Pyrrolidines / chemistry*
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Pyrrolidines / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Aminobutyrates
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Dipeptidyl-Peptidase IV Inhibitors
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Hydrocarbons, Fluorinated
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Hypoglycemic Agents
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Protease Inhibitors
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Pyrrolidines
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2-amino-4-phenylbutyric acid
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Dipeptidyl Peptidase 4