| Title : 1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors - Sakashita_2005_Bioorg.Med.Chem.Lett_15_2441 |
| Author(s) : Sakashita H , Kitajima H , Nakamura M , Akahoshi F , Hayashi Y |
| Ref : Bioorganic & Medicinal Chemistry Lett , 15 :2441 , 2005 |
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Abstract :
1-(Gamma-substituted prolyl)-(S)-2-cyanopyrrolidines were designed based on the predicted binding mode of the known DPP-IV inhibitor NVP-DPP728 and evaluated for their inhibitory activity. In structure-activity relationship study at the gamma-position of proline, it became clear that compounds bearing (S)-stereochemistry were 20-fold more potent than the antipode. Of these compounds, the (3,4-dicyanophenyl)amino- and (3-chloro-4-cyanophenyl)amino-derivatives showed the highest inhibitory activity. |
| PubMedSearch : Sakashita_2005_Bioorg.Med.Chem.Lett_15_2441 |
| PubMedID: 15863294 |
Sakashita H, Kitajima H, Nakamura M, Akahoshi F, Hayashi Y (2005)
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors
Bioorganic & Medicinal Chemistry Lett
15 :2441
Sakashita H, Kitajima H, Nakamura M, Akahoshi F, Hayashi Y (2005)
Bioorganic & Medicinal Chemistry Lett
15 :2441