1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
| Autor: | Bernd Kuhn, Hans Peter Wessel, Jens-Uwe Peters, Patrizio Mattei, Robert Narquizian, Pierre C. Wyss, Luca Gobbi, Daniel Hunziker, Thomas Lübbers, Bernd Michael Löffler, Markus Bohringer, Yves Ruff, Michael Hennig |
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| Rok vydání: | 2007 |
| Předmět: |
Dipeptidyl-Peptidase IV Inhibitors
biology Adenosine Deaminase Protein Conformation Stereochemistry Chemistry Dipeptidyl Peptidase 4 Organic Chemistry Clinical Biochemistry Pharmaceutical Science Quinolizine Biochemistry Chemical synthesis Structure-Activity Relationship Piperidines Enzyme inhibitor Drug Discovery Adenosine Deaminase Inhibitors biology.protein Humans Molecular Medicine Protease Inhibitors Molecular Biology Glycoproteins |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:2966-2970 |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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