1,3-Disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors

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 th...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (11), p.2966-2970
Main Authors: Lübbers, Thomas, Böhringer, Markus, Gobbi, Luca, Hennig, Michael, Hunziker, Daniel, Kuhn, Bernd, Löffler, Bernd, Mattei, Patrizio, Narquizian, Robert, Peters, Jens-Uwe, Ruff, Yves, Wessel, Hans Peter, Wyss, Pierre
Format: Article
Language:English
Subjects:
2-Aminobenzo-[a]quinolizine
Adenosine Deaminase - chemistry
Adenosine Deaminase Inhibitors
Biological and medical sciences
Dipeptidyl Peptidase 4 - chemistry
Dipeptidyl peptidase IV
Dipeptidyl-Peptidase IV Inhibitors
DPP-IV inhibitor
General and cellular metabolism. Vitamins
Glycoproteins - antagonists & inhibitors
Glycoproteins - chemistry
Humans
Medical sciences
Pharmacology. Drug treatments
Piperidines - chemical synthesis
Piperidines - chemistry
Piperidines - pharmacology
Protease Inhibitors - chemical synthesis
Protease Inhibitors - chemistry
Protease Inhibitors - pharmacology
Protein Conformation
Structure-Activity Relationship
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Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.03.072