| Title : Synthesis and structure-activity relationships of potent 1-(2-substituted-aminoacetyl)-4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors - Fukushima_2008_Chem.Pharm.Bull.(Tokyo)_56_1110 |
| Author(s) : Fukushima H , Hiratate A , Takahashi M , Saito-Hori M , Munetomo E , Kitano K , Saito H , Takaoka Y , Yamamoto K |
| Ref : Chem Pharm Bull (Tokyo) , 56 :1110 , 2008 |
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Abstract :
Dipeptidyl peptidase IV (DPP-IV) inhibitors have attracted attention as potential drugs for use in the treatment of type 2 diabetes because they prevent the degradation of glucagon-like peptide-1 (GLP-1) and extend its duration of action. We previously reported that 2-cyano-4-fluoropyrrolidines act as potent DPP-IV inhibitors and have been modifying the 1-position of pyrrolidine to obtain more useful inhibitors. An L-tert-butylglycine derivative was found to be a stable and potent DPP-IV inhibitor that exhibits a glucose lowering effect in vivo. Here, we report the synthesis of and biological data on the aforementioned derivatives. |
| PubMedSearch : Fukushima_2008_Chem.Pharm.Bull.(Tokyo)_56_1110 |
| PubMedID: 18670111 |
Fukushima H, Hiratate A, Takahashi M, Saito-Hori M, Munetomo E, Kitano K, Saito H, Takaoka Y, Yamamoto K (2008)
Synthesis and structure-activity relationships of potent 1-(2-substituted-aminoacetyl)-4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors
Chem Pharm Bull (Tokyo)
56 :1110
Fukushima H, Hiratate A, Takahashi M, Saito-Hori M, Munetomo E, Kitano K, Saito H, Takaoka Y, Yamamoto K (2008)
Chem Pharm Bull (Tokyo)
56 :1110