The study aimed to investigate 12 novel thiazole compounds in the treatment of neurodegenerative disorders. The compounds produced were evaluated for their inhibitory efficacy against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and monoamine oxidases (MAOs). Among the compounds, , , and showed the highest AChE inhibitory activity. The IC values for compounds are 0.223 ± 0.010 µM, 0.092 ± 0.003 µM, and 0.054 ± 0.002 µM, respectively. In addition, molecular docking analyses and molecular dynamic simulation were used to examine the interactions of these compounds with protein sites. The results suggest that thiazole-ring compounds could serve as a promising basis for the development of drugs aimed at treating neurodegenerative diseases (NDD), caused by Parkinson's and Alzheimer's diseases.
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http://dx.doi.org/10.1080/07391102.2024.2437521 | DOI Listing |
Sci Rep
December 2024
Department of Zoology, Biomedical Technology, Human Genetics, and WBC, School of Sciences, Gujarat University, Ahmedabad, 380009, Gujarat, India.
Ovarian cancer is known to be a challenging disease to detect at an early stage and is a major cause of death among women. The current treatment for ovarian cancer typically involves a combination of surgery and the use of drugs such as platinum-based cytotoxic agents, anti-angiogenic drugs, etc. However, current treatment methods are not always effective in preventing the recurrence of ovarian cancer.
View Article and Find Full Text PDFJ Nat Prod
December 2024
State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China.
-Terphenyl compounds are known to possess a diverse range of biological activities, making the synthesis of novel -terphenyl derivatives a significant research objective. In this study, we report the first synthesis of nocarterphenyl A (), characterized by a thiazole-fused -terphenyl framework. Furthermore, we synthesized 18 additional analogs, including the naturally occurring compound 5-methoxy-4,7-bis(4-methoxyphenyl)benzo[]thiazol-6-ol (), employing a similar synthetic approach.
View Article and Find Full Text PDFMikrochim Acta
December 2024
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming, 650500, People's Republic of China.
A novel copper and iron doped containing chitosan and heparin sodium carbon dots (CS-Cu,Fe/HS) nanozyme was formulated through a single-step microwave digestion method. CS-Cu,Fe/HS exhibits excellent peroxidase (POD)-like activity and positive charge characteristics, and it can oxidize the negatively charged 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) in the presence of HO to produce a green compound (ox-ABTS). Furthermore, CS-Cu,Fe/HS enhances electron transfer and provides additional active sites through the valence state transformations of Fe/Fe and Cu/Cu.
View Article and Find Full Text PDFBiosensors (Basel)
December 2024
LAQV, REQUIMTE, Department of Chemical Sciences, Laboratory of Applied Chemistry, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira n° 228, 4050-313 Porto, Portugal.
Accurate and selective monitoring of thiamine levels in multivitamin supplements is essential for preventing deficiencies and ensuring product quality. To achieve this, a Förster resonance energy transfer (FRET) system using carbon dots (CDs) as energy donors and citrate-stabilized silver nanoparticles (AgNPs) as energy acceptors was developed. The aqueous synthesis of AgNPs using microwave irradiation was optimized to obtain efficient plasmonic nanoparticles for FRET applications, targeting maximal absorbance intensity, stability, and wavelength alignment.
View Article and Find Full Text PDFFuture Med Chem
December 2024
Chemistry Department, Faculty of science(Girls), Al-Azhar University, Nasr City, Cairo, Egypt.
Aim: Emerging resistance among pathogens necessitates the development of novel antimicrobial agents. As a result, we aimed to synthesize new coumarins and study their antimicrobial activity with the hope of obtaining effective drugs.
Method: A series of coumarins were synthesized, characterized, and assessed for antimicrobial activity using broth microdilution and agar diffusion methods against Gram-positive (), Gram-negative () bacteria, and fungi ().
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