| Title : 1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors - Lubbers_2007_Bioorg.Med.Chem.Lett_17_2966 |
| Author(s) : Lubbers T , Bohringer M , Gobbi L , Hennig M , Hunziker D , Kuhn B , Loffler B , Mattei P , Narquizian R , Peters JU , Ruff Y , Wessel HP , Wyss P |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2966 , 2007 |
|
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. |
| PubMedSearch : Lubbers_2007_Bioorg.Med.Chem.Lett_17_2966 |
| PubMedID: 17418568 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | GVB |
| Gene_locus | human-DPP4 |
| Structure | 2JID |
Lubbers T, Bohringer M, Gobbi L, Hennig M, Hunziker D, Kuhn B, Loffler B, Mattei P, Narquizian R, Peters JU, Ruff Y, Wessel HP, Wyss P (2007)
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :2966
Lubbers T, Bohringer M, Gobbi L, Hennig M, Hunziker D, Kuhn B, Loffler B, Mattei P, Narquizian R, Peters JU, Ruff Y, Wessel HP, Wyss P (2007)
Bioorganic & Medicinal Chemistry Lett
17 :2966