Abstract
anti-Substituted beta-methylphenylalanine derived amides have been shown to be potent DPP-IV inhibitors exhibiting excellent selectivity over both DPP8 and DPP9. The optimized compound exhibited good pharmacokinetic profiles in three preclinical species.
MeSH terms
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Adenosine Deaminase / metabolism
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Adenosine Deaminase Inhibitors*
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Administration, Oral
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Amides / chemistry
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Animals
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Biological Availability
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Dipeptidyl Peptidase 4 / metabolism
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Dogs
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Glycoproteins / antagonists & inhibitors*
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Glycoproteins / metabolism
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Humans
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Inhibitory Concentration 50
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Macaca mulatta
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Molecular Structure
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Nitrogen / chemistry
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Protease Inhibitors / administration & dosage*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacokinetics
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Protease Inhibitors / pharmacology*
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Pyridones / administration & dosage*
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Pyridones / chemistry
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Pyridones / pharmacokinetics
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Pyridones / pharmacology*
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Rats
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Sensitivity and Specificity
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Adenosine Deaminase Inhibitors
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Amides
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Glycoproteins
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Protease Inhibitors
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Pyridones
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DPP4 protein, human
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Dipeptidyl Peptidase 4
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Adenosine Deaminase
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Nitrogen