Design, synthesis and biological evaluation of novel DPP-IV inhibitors

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 cruc...

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Bibliographic Details
Published inJournal of the Indian Chemical Society Vol. 97; no. 8; pp. 1227 - 1235
Main Authors Karelia, Chirag, Parmar, Kailash, Teli, Divya, Chhabria, Mahesh
Format Journal Article
LanguageEnglish
Published JODHPUR Scientific Publ-India 01.08.2020
Subjects
Chemistry
Chemistry, Multidisciplinary
Physical Sciences
Science & Technology
Type 2 diabetes
virtual screening
3D QSAR pharmacophore
N,N-acetal
S,N-acetal
DERIVATIVES
DPP-IV inhibitor
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Summary: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 mu M.
ISSN:0019-4522