| Title : Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors - Fukushima_2008_Bioorg.Med.Chem_16_4093 |
| Author(s) : Fukushima H , Hiratate A , Takahashi M , Mikami A , Saito-Hori M , Munetomo E , Kitano K , Chonan S , Saito H , Suzuki A , Takaoka Y , Yamamoto K |
| Ref : Bioorganic & Medicinal Chemistry , 16 :4093 , 2008 |
| Abstract : Dipeptidyl peptidase IV (DPP-IV) inhibitors are promising antidiabetic drugs, and several drugs are in the developmental stage. We previously reported that the introduction of fluorine to the 4-position of 2-cyanopyrrolidine enhanced the DPP-IV inhibitory effect. In the present report, we examined the structure-activity relationship (SAR) of 2-cyano-4-fluoropyrrolidine with N-substituted glycine at the 1-position. We report the identification of a potent and stable DPP-IV inhibitor (TS-021) with a long-term persistent plasma drug concentration and a potent antihyperglycemic activity. |
| ESTHER : Fukushima_2008_Bioorg.Med.Chem_16_4093 |
| PubMedSearch : Fukushima_2008_Bioorg.Med.Chem_16_4093 |
| PubMedID: 18243000 |
Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K (2008)
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry
16 :4093
Fukushima H, Hiratate A, Takahashi M, Mikami A, Saito-Hori M, Munetomo E, Kitano K, Chonan S, Saito H, Suzuki A, Takaoka Y, Yamamoto K (2008)
Bioorganic & Medicinal Chemistry
16 :4093