Abstract
The induction of conformationally restricted N-(aryl or heteroaryl)-3-azabicyclo[3.1.0]hexane derivatives at P(2) region of compounds of 2-cyanopyrrolidine class was explored to develop novel DPP-IV inhibitors. The synthesis, structure-activity relationship, and selectivity against related proteases are delineated.
MeSH terms
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Amino Acid Motifs
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Bridged Bicyclo Compounds, Heterocyclic / chemistry*
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology
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Cell Proliferation / drug effects
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Chemistry, Pharmaceutical / methods
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Diabetes Mellitus, Type 2 / drug therapy
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Diabetes Mellitus, Type 2 / therapy
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Dipeptidyl Peptidase 4 / chemistry
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Dipeptidyl-Peptidase IV Inhibitors*
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Drug Design
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Hexanes / chemistry*
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Hexanes / pharmacology
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Humans
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Ligands
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Models, Chemical
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Molecular Conformation
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Piperidines / chemistry
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Protease Inhibitors / chemistry*
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Protease Inhibitors / pharmacology*
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Structure-Activity Relationship
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T-Lymphocytes / drug effects*
Substances
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3-azabicyclo(3.1.0)hexane
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Bridged Bicyclo Compounds, Heterocyclic
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Dipeptidyl-Peptidase IV Inhibitors
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Hexanes
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Ligands
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Piperidines
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Protease Inhibitors
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Dipeptidyl Peptidase 4