Abstract
In a search for novel DPP-IV inhibitors, 2-aminobenzo[a]quinolizines were identified as submicromolar HTS hits. Due to the difficult synthetic access to this compound class, 1,3-disubstituted 4-aminopiperidines were used as model compounds for optimization. The developed synthetic methodology and the SAR could be transferred to the 2-aminobenzo[a]quinolizine series, leading to highly active DPP-IV inhibitors.
MeSH terms
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Adenosine Deaminase / chemistry
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Adenosine Deaminase Inhibitors*
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Dipeptidyl Peptidase 4 / chemistry
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Dipeptidyl-Peptidase IV Inhibitors*
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Glycoproteins / antagonists & inhibitors*
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Glycoproteins / chemistry
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Humans
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / 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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Protein Conformation
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Structure-Activity Relationship
Substances
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Adenosine Deaminase Inhibitors
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Dipeptidyl-Peptidase IV Inhibitors
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Glycoproteins
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Piperidines
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Protease Inhibitors
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N-aminopiperidine
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DPP4 protein, human
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Dipeptidyl Peptidase 4
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Adenosine Deaminase