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Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives Publisher



Firoozpour L1 ; Kazemzadeh Arasi F2 ; Toolabi M3 ; Moghimi S1 ; Armandeh M4 ; Salmani F5 ; Pakrad R5 ; Firuzpour H5 ; Ghasemi Dogaheh M6 ; Ebrahimi SES2 ; Hme Ketabforoosh S7 ; Karima S5 ; Foroumadi A1, 2
Authors

Source: Medicinal Chemistry Research Published:2023


Abstract

In this paper, pyridazin derivatives containing different thiobenzyl moieties were synthesized and screened for their inhibitory activities against rat intestinal α-glucosidase enzyme. The final products were easily obtained without the need to harsh purification steps. The in vitro results revealed that all the synthesized compounds were more potent (IC50s = 26.3–148.9 μM) than the clinically used drug, acarbose. The kinetic study revealed the competitive inhibition behavior of compound 5m (Ki = −56 μM). Docking studies showed imperative interactions such as hydrogen bonding, Pi-Pi T-shaped, and Pi-anion interactions confirming the observed activity. The RMSD value was determined less than 3 A and validated the study. Graphical Abstract: [Figure not available: see fulltext.] © 2023, The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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