کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378905 | 982014 | 2005 | 5 صفحه PDF | دانلود رایگان |

1-(γ-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 γ-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.
1-((S)-γ-Substituted prolyl)-(S)-2-cyanopyrrolidine was found to be suitable structure for DPP-IV inhibition. Of these, (3,4-dicyanophenyl)amino-(17f) and (3-chloro-4-cyanophenyl)amino-derivatives (17g) showed the highest inhibitory activity.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2441–2445