Boehringer, M. and Fischer, H. and Hennig, M. and Hunziker, D. and Huwyler, J. and Kuhn, B. and Loeffler, B. M. and Luebbers, T. and Mattei, P. and Narquizian, R. and Sebokova, E. and Sprecher, U. and Wessel, H. P.. (2010) Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors. Bioorganic & medicinal chemistry letters, Vol. 20, H. 3. pp. 1106-1108.
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Official URL: http://edoc.unibas.ch/dok/A5840963
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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.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler) |
|---|---|
| UniBasel Contributors: | Huwyler, Jörg |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Pergamon |
| ISSN: | 0960-894X |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Last Modified: | 08 Jun 2012 06:56 |
| Deposited On: | 08 Jun 2012 06:51 |
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