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Bicyclic cyanothiazolidines as novel dipeptidyl peptidase 4 inhibitors |
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| Authors: | Juan M. Betancort David T. Winn Ruzhang Liu Quansheng Xu Junjuan Liu Wensheng Liao Shu-Hui Chen David Carney Denise Hanway James Schmeits Xinqiang Li Eric Gordon David A. Campbell |
| Affiliation: | 1. Phenomix Corporation, 5871 Oberlin Drive, Suite 200, San Diego, CA 92121, USA;2. WuXi AppTec, Inc., No. 1 Building, 288 FuTe ZhongLu, Shanghai 200131, China |
| Abstract: | The synthesis and biochemical evaluation of novel cyanothiazolidine inhibitors of dipeptidyl peptidase 4 (DPP4) is described. Their main structural feature is a constrained bicyclic core that prevents the intramolecular formation of inactive cyclic species. The inhibitors show good to moderate biochemical potency against DPP4 and display distinct selectivity profiles towards DPP7, DPP8 and DPP9 depending on their substitution. |
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