| 17317162 |
Yoshida T, Sakashita H, Akahoshi F, Hayashi Y: [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl] thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors. Bioorg Med Chem Lett. 2007 May 1;17(9):2618-21. Epub 2007 Feb 8.
In the search for an inhibitor of dipeptidyl peptidase IV (DPP-IV) highly potent both in vitro and in vivo, we synthesized a series of L-prolylthiazolidine-based DPP-IV inhibitors having 4-arylpiperazine or 4-arylpiperidine at the gamma-position of the proline structure. Of these compounds, the 4-(5-nitro-2-pyridyl) piperazine analog 21e showed a sub-nanomolar (IC (50)=0.92 nmol/L) DPP-IV inhibitory activity and a long-lasting in vivo DPP-IV inhibition profile. |
83(1,1,1,3) |