A novel biologically active thiosemicarbazide derivative ligand () and a series of its five metal(II) complexes, namely: [Co(L)Cl], [Ni(L)Cl(HO)], [Cu(L)Cl(HO)], [Zn(L)Cl] and [Cd(L)Cl(HO)] have been synthesized and thoroughly investigated. The physicochemical characterization of the newly obtained compounds has been performed using appropriate analytical techniques, such as H and C nuclear magnetic resonance (NMR), inductively coupled plasma (ICP), thermogravimetric analysis (TGA), Fourier-transform infrared spectroscopy (FTIR) and magnetic measurements. In order to study the pharmacokinetic profile of the compounds, ADMET analysis was performed. The in vitro studies revealed that the synthesized compounds exhibit potent biological activity against A549 human cancer cell line.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9100868 | PMC |
http://dx.doi.org/10.3390/molecules27092703 | DOI Listing |
Front Pharmacol
January 2025
Department of Surgical Sciences, Functional Pharmacology and Neuroscience, Uppsala University, Uppsala, Sweden.
Background: Xanthones are dubbed as putative lead-like molecules for cancer drug design and discovery. This study was aimed at the synthesis, characterization, and target fishing of novel xanthone derivatives.
Methods: The products of reactions of xanthydrol with urea, thiourea, and thiosemicarbazide reacted with α-haloketones to prepare the thiazolone compounds.
Sci Rep
January 2025
Natural and Medical Sciences Research Center, University of Nizwa, Birkat Al Mauz, P. O. Box 33, Nizwa, Oman.
Diabetes mellitus, particularly type 2 diabetes, is a growing global health challenge characterized by chronic hyperglycemia due to insulin resistance. One therapeutic approach to managing this condition is the inhibition of α-glucosidase, an enzyme involved in carbohydrate digestion, to reduce postprandial blood glucose levels. In this study, a series of thiosemicarbazide-linked quinoline-piperazine derivatives were synthesized and evaluated for their α-glucosidase inhibitory activity, to identify new agents for type 2 diabetes management.
View Article and Find Full Text PDFMolecules
December 2024
Department of Pharmaceutical Chemistry, Drug Analyses and Radiopharmacy, Faculty of Pharmacy, Medical University of Lodz, 90-151 Lodz, Poland.
This paper presents the synthesis and characterization of new thiosemicarbazone derivatives with potential applications as antibacterial, antioxidant and anticancer agents. Six thiosemicarbazone derivatives (L-L5) were synthesized by reacting an appropriate thiosemicarbazide derivative with 2-pyridinecarboxaldehyde. The structures of the obtained compounds were confirmed using mass spectrometry, infrared spectroscopy, and NMR spectroscopy.
View Article and Find Full Text PDFJ 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 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 PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!