Abstract
To research the structure-activity relationship (SAR) of glycinamide-bearing compounds that used as inhibitors of dipeptidyl peptidase IV (DPP-IV), P32/98 and compound A were chosen as the leading compounds, heterocycles containing nitrogen atom were introduced to form amide, and different residues on a-position of carbonyl were designed. The nineteen designed compounds were synthesized by a simple route and were evaluated as inhibitors of DPP-IV. All of the structures were characterized by 1H NMR and HRMS. The preliminary SAR result was obtained.
Publication types
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English Abstract
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Research Support, Non-U.S. Gov't
MeSH terms
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Dipeptidyl Peptidase 4 / metabolism*
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Dipeptidyl-Peptidase IV Inhibitors / chemical synthesis*
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Dipeptidyl-Peptidase IV Inhibitors / chemistry
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Dipeptidyl-Peptidase IV Inhibitors / pharmacology
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Drug Design
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Glycine / analogs & derivatives*
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Glycine / chemistry
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Magnetic Resonance Spectroscopy / methods
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Molecular Structure
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Piperazines / chemistry
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Piperazines / pharmacology
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Structure-Activity Relationship
Substances
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Dipeptidyl-Peptidase IV Inhibitors
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Piperazines
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glycine amide
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1-ethyl-2,3-dioxopiperazine
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Dipeptidyl Peptidase 4
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Glycine