| Title : Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors - Tsai_2009_Bioorg.Med.Chem.Lett_19_1908 |
| Author(s) : Tsai TY , Hsu T , Chen CT , Cheng JH , Chiou MC , Huang CH , Tseng YJ , Yeh TK , Huang CY , Yeh KC , Huang YW , Wu SH , Wang MH , Chen X , Chao YS , Jiaang WT |
| Ref : Bioorganic & Medicinal Chemistry Lett , 19 :1908 , 2009 |
|
Abstract :
A series of (2S)-cyanopyrrolidines with glutamic acid derivatives at the P2 site have been prepared and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV). The structure-activity relationships (SAR) led to the discovery of potent 3-substituted glutamic acid analogues, providing enhanced chemical stability and excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. Compound 13f exhibited the ability to both significantly decrease the glucose excursion and inhibit plasma DPP-IV activity. |
| PubMedSearch : Tsai_2009_Bioorg.Med.Chem.Lett_19_1908 |
| PubMedID: 19269819 |
Tsai TY, Hsu T, Chen CT, Cheng JH, Chiou MC, Huang CH, Tseng YJ, Yeh TK, Huang CY, Yeh KC, Huang YW, Wu SH, Wang MH, Chen X, Chao YS, Jiaang WT (2009)
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
19 :1908
Tsai TY, Hsu T, Chen CT, Cheng JH, Chiou MC, Huang CH, Tseng YJ, Yeh TK, Huang CY, Yeh KC, Huang YW, Wu SH, Wang MH, Chen X, Chao YS, Jiaang WT (2009)
Bioorganic & Medicinal Chemistry Lett
19 :1908