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Comparative Study
. 2010 Feb 1;20(3):1106-8.
doi: 10.1016/j.bmcl.2009.12.025. Epub 2009 Dec 6.

Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors

Markus Boehringer  1 , Holger Fischer, Michael Hennig, Daniel Hunziker, Joerg Huwyler, Bernd Kuhn, Bernd M Loeffler, Thomas Luebbers, Patrizio Mattei, Robert Narquizian, Elena Sebokova, Urs Sprecher, Hans Peter Wessel
Affiliations
Comparative Study

Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors

Markus Boehringer et al. Bioorg Med Chem Lett. .

Abstract

Synthesis and SAR are described for a structurally distinct class of DPP-IV inhibitors based on aminobenzo[a]quinolizines bearing (hetero-)aromatic substituents in the S1 specificity pocket. The m-(fluoromethyl)-phenyl derivative (S,S,S)-2g possesses the best fit in the S1 pocket. However, (S,S,S)-2i, bearing a more hydrophilic 5-methyl-pyridin-2-yl residue as substituent for the S1 pocket, displays excellent in vivo activity and superior drug-like properties.

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