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Design, synthesis and biological evaluation of novel DPP-IV inhibitors
Author : Chirag Karelia, Kailash Parmar, Divya Teli and Mahesh Chhabria*
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ABSTRACT
Diabetes mellitus is one of the top ten leading causes of death worldwide. DPP-IV inhibition became an attractive target in controlling type 2 diabetes. Because of the several adverse effects associated with current DPP-IV inhibitors, the discovery and development of newer DPP-IV inhibitors are crucial. Ligand-based 3D QSAR pharmacophore modeling method was used in recognizing the important molecular chemical features of potent DPP-IV inhibitors. The best pharmacophore model (Hypo 1) was generated using HypoGen algorithm of Discovery Studio 2.1 (DS). Based on the Hypo 1 model, four novel designed compounds were synthesized, characterized and screened for their DPP-IV inhibitory potentials. All the compounds (9), (10), (11) and (12) showed IC50 values ranging from 0.035–0.35 μM.
KEYWORD
Type 2 diabetes, DPP-IV inhibitor, 3D QSAR pharmacophore, virtual screening, S,N-acetal, N,N-acetal