Synthesis, in vitro and in silico study of novel 1,3-diphenylurea derived Schiff bases as competitive α-glucosidase inhibitors

Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized an...

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Bibliographic Details
Published in:RSC advances 2024-09, Vol.14 (40), p.29288-29300
Main Authors: Pasha, Anam Rubbab, Ullah, Saeed, Khan, Ajmal, Halim, Sobia Ahsan, Hussain, Javid, Rehman, Tanzila, Talib, Rimsha, Alharthy, Rima D, Kashtoh, Hamdy, Abdellattif, Magda H, Al-Harrasi, Ahmed, Shafiq, Zahid
Format: Article
Language:English
Subjects:
Cataracts
Chemistry
Diabetes mellitus
Glucosidase
Heart diseases
Imines
Metabolic disorders
Public health
Renal function
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Summary:Diabetes mellitus has become a major global health burden because of several related consequences, including heart disease, retinopathy, cataracts, metabolic syndrome, collapsed renal function, and blindness. In the recent study, thirty Schiff base derivatives of 1,3-diphenylurea were synthesized and their anti-diabetic activity was evaluated by targeting α-glucosidase. The compounds exhibited an overwhelming inhibitory potential for α-glucosidase with higher potency ranging from 2.49-37.16 μM. The most effective compound, 5h, showed competitive inhibition of α-glucosidase ( = 3.96 ± 0.0048 μM) in the kinetic analysis and strong binding interactions with key residues α-glucosidase in docking analysis, indicating its potential for better glycemic control in diabetes patients.
ISSN:2046-2069
2046-2069
DOI:10.1039/d4ra05767h