Synthesis, Structure–Activity Relationship, and Pharmacophore Modeling Studies of Pyrazole??3??Carbohydrazone Derivatives as Dipeptidyl Peptidase IV Inhibitors

…, W Wang, Y Tang, H Jiang, J Huang…

Index: Wu, Deyan; Jin, Fangfang; Lu, Weiqiang; Zhu, Jin; Li, Cui; Wang, Wei; Tang, Yun; Jiang, Hualiang; Huang, Jin; Liu, Guixia; Li, Jian Chemical Biology and Drug Design, 2012 , vol. 79, # 6 p. 897 - 906

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Citation Number: 13

Abstract

Type 2 diabetes mellitus (T2DM) is a metabolic disease and a major challenge to healthcare systems around the world. Dipeptidyl peptidase IV (DPP-4), a serine protease, has been rapidly emerging as an effective therapeutic target for the treatment for T2DM. In this study, a series of novel DPP-4 inhibitors, featuring the pyrazole-3-carbohydrazone scaffold, have been discovered using an integrated approach of structure-based virtual screening, ...