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SYNTHESIS OF PHENYLPYRIDINE DERIVATIVES AND THEIR BIOLOGICAL EVALUATION TOWARD DIPEPTIDYL PEPTIDASE-4

Yan Zhu, Xiangguo Meng, Zhengyan Cai, Qun Hao, Weicheng Zhou
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Abstract


A novel series of pyridine-based derivatives was synthesized and evaluated for their inhibitory activity against dipeptidyl peptidase-4 (DPP4). 5-Aminomethyl-6-(2,4-dichlorophenyl)-4-[(1H-1,2,4-triazol-1-yl)methyl]pyridine-2-carboxylic acid was identified as a potent (IC50 0.57 nM) and selective DPP4 inhibitor (DPP8 / DPP4 = 238). A docking study of this compound revealed a hydrogen-bonding interaction with the Arg125 residue of the enzyme providing a potential target residue for further structural optimization.

Keywords


DPP4 inhibitors; phenylpyridines; type 2 diabetes mellitus

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