Category Ranking

98%

Total Visits

921

Avg Visit Duration

2 minutes

Citations

20

Article Abstract

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://www.ncbi.nlm.nih.gov/pmc/articles/PMC11731264PMC
http://dx.doi.org/10.1080/17568919.2024.2432303DOI Listing

Publication Analysis

Top Keywords

urease α-glucosidase
20
inhibitors urease
8
molecular docking
8
compounds
7
urease
5
α-glucosidase
5
assessment thiazole-thiazolidinone
4
thiazole-thiazolidinone derivatives
4
derivatives selective
4
selective inhibitors
4

Similar Publications

Ammonia volatilization from livestock manure is driven by urease-catalyzed urea hydrolysis, strongly influenced by temperature and pH. This study assessed the inhibition performance of phenyl phosphorodiamidate (PPDA) and N-(n-butyl)thiophosphoric triamide (NBPT) under conditions (10-35°C, pH 6-10) representative of manure storage. PPDA achieved strong suppression at 10°C and pH 6, reducing ammonia below 7.

View Article and Find Full Text PDF

Long-term compost fertilization enhanced soil disease suppressiveness by fostering interactions between root exudates and the rhizosphere microbiome.

Microbiol Res

September 2025

College of Resources and Environmental Science, State Key laboratory of nutrient use and management, China Agricultural University, Beijing 100193, China. Electronic address:

A comprehensive understanding of the interplay between agricultural practices and the rhizosphere microbiome particularly the role of root exudates is essential for harnessing microbial potential in sustainable agriculture. In this study, we investigated how disease-suppressive soil alters root exudate profiles in pepper plants and how these elevated exudates influence rhizosphere microbiome assembly and modulate the antagonistic activity of Bacillus methylotrophicus 400 (BM400) against Phytophthora capsici. GC-MS analysis identified distinct compositional profiles of root exudates in the disease-suppressive soil, with marked enrichment of seven compounds.

View Article and Find Full Text PDF

Novel chromogenic medium-based method for the rapid detection of drug resistance.

World J Gastroenterol

August 2025

Guangxi Zhuang Autonomous Region Engineering Research Center of Clinical Prevention and Control Technology and Leading Drug for Microorganisms with Drug Resistance in Border Ethnic Areas, Youjiang Medical University for Nationalities, Baise 533000, Guangxi Zhuang Autonomous Region, China.

Background: (), a globally prevalent pathogen, is exhibiting increasing rates of antimicrobial resistance. However, clinical implementation of pre-treatment susceptibility testing remains limited due to the organism's fastidious growth requirements and prolonged culture time.

Aim: To propose a novel detection method utilizing antibiotic-supplemented media to inhibit susceptible strains, while resistant isolates were identified through urease-mediated hydrolysis of urea, inducing a phenol red color change for visual confirmation.

View Article and Find Full Text PDF

eradication: developing antibiotic-independent antimicrobial moieties.

Crit Rev Microbiol

September 2025

Department of Gastroenterology, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.

( infection is a common and serious infectious disease that requires eradication as it is the primary cause of gastric adenocarcinoma. However, the growing prevalence of antibiotic resistance, severe side effects, and the inability of current treatments to effectively address biofilm-embedded, intracellular, and dormant strains, alongside their long-term gut microbiome disruptions, have rendered standard therapies increasingly ineffective. This predicament underscores the pressing need to explore antibiotic-independent antimicrobial moieties.

View Article and Find Full Text PDF

Background Although infection is a primary risk factor for gastric cancer (GC), the specific bacterial components that causally drive carcinogenesis remain poorly understood. Traditional epidemiological studies are limited by confounding variables and the potential for reverse causation. This study aimed to dissect the causal effects of host antibody responses to various antigens on GC risk using Mendelian randomization (MR).

View Article and Find Full Text PDF