| Title : [(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors - Yoshida_2007_Bioorg.Med.Chem.Lett_17_2618 |
| Author(s) : Yoshida T , Sakashita H , Akahoshi F , Hayashi Y |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2618 , 2007 |
|
Abstract :
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. |
| PubMedSearch : Yoshida_2007_Bioorg.Med.Chem.Lett_17_2618 |
| PubMedID: 17317162 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | CHEMBL2147710 CHEMBL2058971 Teneligliptin |
| Gene_locus | human-DPP4 |
| Structure | 3VJK 3VJL 3VJM |
Yoshida T, Sakashita H, Akahoshi F, Hayashi Y (2007)
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :2618
Yoshida T, Sakashita H, Akahoshi F, Hayashi Y (2007)
Bioorganic & Medicinal Chemistry Lett
17 :2618