Boehringer_2010_Bioorg.Med.Chem.Lett_20_1106

Reference

Title : Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors - Boehringer_2010_Bioorg.Med.Chem.Lett_20_1106
Author(s) : 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
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :1106 , 2010
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.

PubMedSearch : Boehringer_2010_Bioorg.Med.Chem.Lett_20_1106
PubMedID: 20031408
Gene_locus related to this paper: human-DPP4

Related information

Inhibitor 23Q
Gene_locus 23Q    human-DPP4
Structure 23Q    human-DPP4    3KWJ

Citations formats

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 (2010)
Aryl- and heteroaryl-substituted aminobenzo[a]quinolizines as dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett 20 :1106

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 (2010)
Bioorganic & Medicinal Chemistry Lett 20 :1106