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Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes |
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| Authors: | Tang Peng Cho Yang Fang Long Lin Zhi Gang Wang Yang Lu He Jun Shen Guang Yuan Fu Jian Hong Wang Lin Guan Dong Liang Zhang Lei Luo Jing Jing Gong Ai Shen She Gao Hong Wang Dan Feng Ying Yan Pang Ke Leng Ying Feng Jun Mong Xian Tai |
| Affiliation: | 1. Shanghai Hengrui Pharmaceuticals Co., Ltd, 279 Wenjing Road, Shanghai 200245, China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China |
| Abstract: | A series of novel azobicyclo[3.3.0]octane derivatives were synthesized and evaluated as dipeptidyl peptidase 4 (DPP-4) inhibitors. The effort resulted in the discovery of inhibitor 2a, which exhibited excellent efficacies in an oral glucose tolerance test. Introduction of methyl group (2j) could prolong the inhibition of serum DPP-4 activity. |
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