Aims: Current research work aims to synthesize hybrid compounds with a thiazole-thiazolidinone structure, as potent inhibitors of urease and α-glucosidase enzymes.
Materials And Methods: These compounds were characterize throughHNMR,CNMR and HREI-MS techniques. These compounds were also evaluated for their potential to inhibit urease and α-glucosidase enzymes for the treatment of urinary tract infections (UTIs) and diabetes treatments. Moreover, molecular docking and ADMET analysis was carried out to confirm biological outcomes.
Results And Conclusion: Compounds-4 (IC = 1.80 ± 0.80 and 3.61 ± 0.59 μM against urease and α-glucosidase, respectively) exhibited significant effectiveness in inhibiting the activity of both enzymes in comparison to the conventional inhibitors thiourea and acarbose. Molecular docking experiments showed that potent compounds exhibited favorable binding orientations in the active sites of urease and α-glucosidase playing a pivotal role in inhibition profile of these compounds. These compounds were also investigated for their drug likeness and were found with desirable attributes for pharmaceutical development. Based on the findings of this research, these compounds have the potential to be developed into effective anti-diabetic and anti-urease treatments in the future.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1080/17568919.2024.2432303 | DOI Listing |
J Fungi (Basel)
December 2024
Agricultural College, Yanbian University, Yanji 133002, China.
Cucumber wilt disease, caused by f. sp. (FOC), is a major threat to cucumber production, especially in greenhouses.
View Article and Find Full Text PDFMar Drugs
November 2024
Nuclear Research Centre of Birine, Ain Oussera 17200, Algeria.
This study represents the first investigation into the ultrasonic and microwave extraction of bioactive metabolites from (red seaweed) and () (brown seaweed), with a focus on their biological activities. The research compares ultrasound-assisted extraction (UAE) with microwave-assisted extraction (MAE) utilizing a hydromethanolic solvent to evaluate their effects on these seaweeds' bioactive compounds and biological activities. The assessment included a series of antioxidant essays: DPPH, ABTS, phenanthroline, and total antioxidant capacity, followed by enzyme inhibition activities: alpha-amylase and urease.
View Article and Find Full Text PDFVirulence
December 2025
The Conway Institute of Biomolecular and Biomedical Science, University College Dublin, Dublin, Ireland.
Infection with is one of the most common infections of mankind. Infection typically occurs in childhood and persists for the lifetime of the host unless eradicated with antimicrobials. The organism colonizes the stomach and causes gastritis.
View Article and Find Full Text PDFFood Sci Nutr
December 2024
Food Quality Control and Analysis Program, Ula Ali Kocman Vocational School Mugla Sitki Kocman University Ula Mugla Turkey.
The current study aims to prepare a green extract using a new method in addition to conventional extraction methods including; methanolic and ultrasonic extraction of , to compare their phenolic composition utilizing high-performance liquid chromatograph equipped with a diode array detector (HPLC-DAD), anti-bacterial, anti-oxidant, and enzyme inhibition activities. The results of HPLC-DAD analysis showed that Rosmarinic acid was found the highest amount in the methanolic extract followed by ultrasonic and green extracts as 169.7 ± 0.
View Article and Find Full Text PDFScand J Gastroenterol
December 2024
Department of clinical and molecular medicine, Norwegian University of Science and Technology, Trondheim, Norway.
Aims: , the dominating cause of gastric cancer, most often infects children initiating inflammation in the antral part and spreads orally to the oxyntic mucosa. Traditionally, eradication of has been based upon a combination of antibiotics together with a proton pump inhibitor (PPI) to reduce gastric destruction of the antibiotics. Recently it has been shown that the more efficient inhibitors of acid secretion, the potassium-competitive acid blockers (PCABs) in combination with amoxicillin alone gave highly sufficient eradication.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!