Discovery of novel 1,3,5-triazine derivatives as an antidiabetic agent in Wistar rats via inhibition of DPP-4

Author:

Gupta Akanksha12,Bhat Hans Raj3ORCID,Singh Udaya Pratap1ORCID

Affiliation:

1. Department of Pharmaceutical Sciences, Drug Design & Discovery Laboratory, Shalom Institute of Health and Allied Sciences (SIHAS), Sam Higginbottom University of Agriculture, Technology and Sciences (SHUATS), Prayagraj, Uttar Pradesh, 211007, India

2. United Institute of Pharmacy, Prayagraj, Uttar Pradesh, 211008, India

3. Department of Pharmaceutical Sciences, Dibrugarh University, Dibrugarh Assam, 786004, India

Abstract

Aim: To develop imeglimin-inspired novel 1,3,5-triazine derivatives as antidiabetic agents. Materials & methods: These derivatives were synthesized and tested against DPP enzymes. Compound 8c was tested for in vivo antidiabetic activity in streptozotocin-induced diabetes in Wistar rats by estimating various biochemical parameters. Docking experiments were also performed. Results: Compound 8c was identified as a selective and potent DPP-4 inhibitor. It was proficiently docked into the catalytic triad of Ser 630, Asp 710 and His740 in S1 and S2 pockets of DPP-4. In experimental animals, it also showed dose-dependent improvement in blood glucose, blood insulin, bodyweight, lipid profile and kidney and liver antioxidant profiles. Conclusion: This study demonstrated the discovery of imeglimin-inspired novel 1,3,5-triazines as a potent antidiabetic agent.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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