887283-36-5Relevant academic research and scientific papers
Design, Synthesis and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel DPP-4 Inhibitors
Li, Qing,Zhou, Muxing,Han, Li,Cao, Qing,Wang, Xinning,Zhao, Leilei,Zhou, Jinpei,Zhang, Huibin
, p. 849 - 856 (2015/10/06)
A new series of DPP-4 inhibitors with imidazo[1,2-a]pyridine scaffold were designed by exploiting scaffold hopping strategy and docking study. Based on docking binding model, structural modifications of 2-benzene ring and pyridine moieties of compound 5a led to the identification of compound 5d with 2, 4-dichlorophenyl group at the 2-position as a potent (IC50 = 0.13 μm), selective (DPP-8/DPP-4 = 215 and DPP-9/DPP-4 = 192) and in vivo efficacious DPP-4 inhibitor. Further, molecular docking revealed that compound 5d could retain key binding features of DPP-4 with the pyridine moiety of imidazo[1,2-a]pyridine ring providing an additional π-π interaction with Phe357 of DPP-4. Compound 5d might be a promising lead for further development of novel DPP-4 inhibitor treating T2DM.
IMIDAZO[1,2-A]PYRIDINE COMPOUNDS, COMPOSITIONS, USES AND METHODS RELATED THERETO
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Page/Page column 54-55, (2008/06/13)
The present invention relates to novel imidazo[1,2- a]pyridine compounds of general formula (I) as well as pharmaceutically acceptable salts thereof; wherein R1, R2, R3 and R4 are as defined in the claims. The c
