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A novel series of β-amino pyrrole-2-carbonitrile derivatives was designed and synthesized based on the three-dimensional binding modes of Denagliptin1 and Sitagliptin2.Using the two important predominant fragments,Compound 31(IC50=0.051 μM) was synthesized and showed moderate DPP4 inhibitory activity,but lower selectivity against DPP8 and DPP9.Therefore,further design and modification to enhance activity and selectivity were focused on the pyrrolidine-2-carbonitrile moiety.