New thiosemicarbazide derivatives 2-6 were synthesised by reacting 2-(ethylsulfanyl)benzohydrazide with various aryl isothiocyanates. The cyclisation of compounds 2-6 under reflux conditions in a basic medium (aqueous NaOH, 4 N) yielded compounds 7-11 that contain a 1,2,4-triazole ring. All of the synthesised compounds were screened for their antioxidant activities. Compounds 2, 3, and 7 showed better radical scavenging in a 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with IC50 values of 1.08, 0.22, and 0.74 µg/mL, respectively, compared to gallic acid (IC50, 1.2 µg/mL). Compound 3 also showed superior results in a ferric reducing antioxidant power (FRAP) assay (3054 µM/100 g) compared to those of ascorbic acid (1207 µM/100 g).
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http://dx.doi.org/10.3390/molecules190811520 | DOI Listing |
J Biomol Struct Dyn
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Biruni University, Istanbul, Türkiye.
The increasing global prevalence of Alzheimer's disease necessitates the development of novel therapeutic approaches. Neurodegenerative diseases are associated with increased oxidative stress and levels of cholinesterase enzymes. Hence, the development of cholinesterase inhibitors and antioxidants may provide neuroprotective effects.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Guangxi Key Laboratory of Tumor Immunology and Microenvironmental Regulation, Guangxi Health Commission Key Laboratory of Tumor Immunology and Receptor-Targeted Drug Basic Research, Guilin Medical University, Huan Cheng North 2nd Road 109, Guilin, 541004, PR China. Electronic address:
Metal-based drugs have been used in the clinical treatment of tumors for over 30 years. However, no metal-based drugs have been clinically approved to treat glioma. Although metal complexes have excellent cytotoxicity, their most critical problem is crossing the blood-brain barrier.
View Article and Find Full Text PDFSpectrochim Acta A Mol Biomol Spectrosc
December 2024
LAQV-REQUIMTE, Department of Chemistry and Biochemistry (DQB), Faculty of Sciences, University of Porto (FCUP), 4169-007 Porto, Portugal. Electronic address:
This work describes the successful design and synthesis of a new fluorescence resonance energy transfer (FRET)-based sensor, denoted as RD1. This sensor incorporates a robust dual-fluorophore design, which combines a rhodamine and a dansyl derivative, functionalized with a thiosemicarbazide group that acts as Hg(II) specific recognition site. A synthetic pathway was developed that allowed the efficient synthesis of RD1 with a remarkable overall yield of 44% over four steps, through microwave-assisted protocols.
View Article and Find Full Text PDFActa Crystallogr C Struct Chem
January 2025
Institute of General and Ecological Chemistry, Faculty of Chemistry, Łódź University of Technology, Żeromskiego 116, 90-924 Łódź, Poland.
Three new thiosemicarbazide derivatives are described in terms of synthesis, structure and biological activity. N'-(Morpholine-4-carbonothioyl)-4-(4-phenylpiperazin-1-yl)picolinohydrazonamide 2-methyltetrahydrofuran hemisolvate, 2CHNOS·CHO, 1, determined at 100 K, has orthorhombic (Pca2) symmetry and exhibits disorder. 4-(4-Phenylpiperazin-1-yl)-N'-(piperidine-1-carbonothioyl)picolinohydrazonamide-dimethylformamide-water (1/1/0.
View Article and Find Full Text PDFEng Microbiol
December 2024
Department of Organic Chemistry, Faculty of Chemistry, Shahid Beheshti University, G.C., Tehran, Iran.
Surface adsorption is a convenient and readily available method for immobilizing enzymes on metal-organic frameworks (MOFs). Metal-organic framework-5 (MOF-5), isoreticular metal-organic frameworks-3 (IRMOF-3), and multivariate analysis of MOF-5/IRMOF-3 (MMI) with a half-amino group (-NH) were prepared in this study. lipase (TLL) was chosen as a commercially available enzyme for immobilization on the surfaces of these MOFs.
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