Abstract
In-house screening of the Merck sample collection identified proline derived homophenylalanine 3 as a DPP-IV inhibitor with modest potency (DPP-IV IC50=1.9 microM). Optimization of 3 led to compound 37, which is among the most potent and selective DPP-IV inhibitors discovered to date.
MeSH terms
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Administration, Oral
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Animals
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Biological Availability
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Dipeptidyl Peptidase 4 / metabolism*
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Humans
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In Vitro Techniques
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Proline / analogs & derivatives*
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Proline / chemical synthesis*
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Proline / chemistry
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Proline / pharmacology
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Protease Inhibitors
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Proline
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Dipeptidyl Peptidase 4