Bioorganic & Medicinal Chemistry Letters 2007-06-01

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

Thomas Lübbers, Markus Böhringer, Luca Gobbi, Michael Hennig, Daniel Hunziker, Bernd Kuhn, Bernd Löffler, Patrizio Mattei, Robert Narquizian, Jens-Uwe Peters, Yves Ruff, Hans Peter Wessel, Pierre Wyss

Index: Bioorg. Med. Chem. Lett. 17(11) , 2966-70, (2007)

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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.