Structural highlights
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
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.
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors.,Boehringer M, Fischer H, Hennig M, Hunziker D, Huwyler J, Kuhn B, Loeffler BM, Luebbers T, Mattei P, Narquizian R, Sebokova E, Sprecher U, Wessel HP Bioorg Med Chem Lett. 2010 Feb 1;20(3):1106-8. Epub 2009 Dec 6. PMID:20031408[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Boehringer M, Fischer H, Hennig M, Hunziker D, Huwyler J, Kuhn B, Loeffler BM, Luebbers T, Mattei P, Narquizian R, Sebokova E, Sprecher U, Wessel HP. Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1106-8. Epub 2009 Dec 6. PMID:20031408 doi:10.1016/j.bmcl.2009.12.025
