ChemInform Abstract: Synthesis and Structure-Activity Relationships of Potent 1-(2-Substituted-aminoacetyl)-4-fluoro-2-cyanopyrrolidine Dipeptidyl Peptidase IV Inhibitors

Autor: Akira Hiratate, Yuji Takaoka, Hidetaka Saito, Koji Yamamoto, Masato Takahashi, Masako Saito-Hori, Eiji Munetomo, Hiroshi Fukushima, Kiyokazu Kitano
Rok vydání: 2009
Předmět:
Zdroj: ChemInform. 40
ISSN: 1522-2667
0931-7597
DOI: 10.1002/chin.200903194
Popis: 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.
Databáze: OpenAIRE