| Title : Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors - Kato_2011_Org.Med.Chem.Lett_1_7 |
| Author(s) : Kato N , Oka M , Murase T , Yoshida M , Sakairi M , Yakufu M , Yamashita S , Yasuda Y , Yoshikawa A , Hayashi Y , Shirai M , Mizuno Y , Takeuchi M , Makino M , Takeda M , Kakigami T |
| Ref : Org Med Chem Lett , 1 :7 , 2011 |
|
Abstract :
Focused structure-activity relationships of isoindoline class DPP-IV inhibitors have led to the discovery of 4b as a highly selective, potent inhibitor of DPP-IV. In vivo studies in Wistar/ST rats showed that 4b was converted into the strongly active metabolite 4l in high yield, resulting in good in vivo efficacy for antihyperglycemic activity. |
| PubMedSearch : Kato_2011_Org.Med.Chem.Lett_1_7 |
| PubMedID: 22373386 |
Kato N, Oka M, Murase T, Yoshida M, Sakairi M, Yakufu M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y, Shirai M, Mizuno Y, Takeuchi M, Makino M, Takeda M, Kakigami T (2011)
Synthesis and pharmacological characterization of potent, selective, and orally bioavailable isoindoline class dipeptidyl peptidase IV inhibitors
Org Med Chem Lett
1 :7
Kato N, Oka M, Murase T, Yoshida M, Sakairi M, Yakufu M, Yamashita S, Yasuda Y, Yoshikawa A, Hayashi Y, Shirai M, Mizuno Y, Takeuchi M, Makino M, Takeda M, Kakigami T (2011)
Org Med Chem Lett
1 :7