Background: Nowadays, acidity is a severe problem worldwide caused by excessive gastric acid secretion by the stomach and proximal intestine.
Objective: Antacids are drugs capable of buffering stomach acid. Therefore, in our research work, we have reported the studies, synthesis, characterization, and evaluation of antacid activities of magnesium (II) complexes via the acid-base neutralization process.
Methods: In this research, some magnesium complexes were synthesized and their antacid behavior was compared with marketed products. Also, studies were performed on H+/K+ ATPase (Proton pump). All synthesized compounds were characterized by various spectroscopic techniques like UV-Vis, FT-IR, XRD, and DSC techniques.
Result: Spectroscopic analysis results showed that the semicarbazone ligand shows keto-enol isomerism and forms a coordinated stable complex with magnesium ions in the crystalline phase. The FT-IR results confirmed the presence of Mg-O stretching, N-H bending, and C=N stretching vibrations in Mg (II) complexes.
Conclusion: The antacid activities of Mg (II) complexes were excellent as compared to the semicarbazone ligand and comparable with that of marketed antacid drugs like ENO, and Pantop-D. Insilco studies also confirmed that semicarbazone ligand and its Mg (II) complexes were both found to be fitted into the active sites of molecular targets, and Mg (II) complexes showed better binding affinities towards macromolecular as compared to semicarbazone ligand.
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http://dx.doi.org/10.2174/0115701638276401240315084143 | DOI Listing |
Eur J Med Chem
January 2025
Institute of Chemistry, Universidade Federal Rural do Rio de Janeiro, Seropédica, 23897-000, Brazil. Electronic address:
Inhibition of cholinesterases, combined with antioxidant activity, metal-chelating capacity, and neuroprotection, is recognized as an effective multitarget therapy for the treatment of Alzheimer's disease (AD). Based on our in-house thiosemicarbazone-acridine compounds, this study recognized these derivatives as possible multi-target-directed ligand (MTDL). Initial screening against cholinesterases identified CL-01, which exhibited a promising IC value of 0.
View Article and Find Full Text PDFJ Am Chem Soc
November 2024
Department of Chemistry and Biomolecular Sciences, University of Ottawa, Ottawa K1N 6N5, Ontario, Canada.
CuATSM, a copper(II) complex of a bis(thiosemicarbazone) of diacetyl, prevents oxidative cell death and acts as a neuroprotectant , prompting its evaluation to treat amyotrophic lateral sclerosis and other neurodegenerative conditions in the clinic. We recently demonstrated that CuATSM functions as a potent radical-trapping antioxidant (RTA), inhibiting lipid peroxidation and associated ferroptotic cell death by a noncanonical mechanism based on radical addition to the ligand backbone. Herein we report our investigations of the generality of this reactivity, which include studies of corresponding complexes of various other metals, including Co, Ru, Ni, Pd, Pt, and Au.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Department of Inorganic Chemistry, School of Sciences, Universidad Autónoma de Madrid (UAM), Madrid, 28049, Spain; Institute for Advance Research in Chemistry UAM, Madrid, 28049, Spain. Electronic address:
Copper(II)-based complexes are promising candidates as anti-cancer agents due to their ability to target cancer cells. Here we describe the synthesis and characterization of two copper(II) thiosemicarbazone complexes with the ligands 4-(dimethylamino)benzaldehyde N4-methylthiosemicarbazone (HL) and 4-(dimethylamino)benzaldehyde N4-(4-(dimethylamino)phenylthiosemicarbazone (HL) and general formula [Cu(L)]. The complexes show stability in aqueous solution with 1 % of DMSO that allows to stablish its solution profile in biological buffers.
View Article and Find Full Text PDFBioorg Chem
December 2024
Faculty of Life Science and Biotechnology, South Asian University, Rajpur Rd, Maidan Garhi, New Delhi 110068, India. Electronic address:
A series of novel modifications were performed at the N(4) position of 5-hydroxyisatin thiosemicarbazone (TSC). The structure-activity approach is applied to design and synthesize derivatives by condensing thiosemicarbazides with 5-hydroxy isatin. The TSCs were characterized by various spectroscopic techniques viz.
View Article and Find Full Text PDFInt J Mol Sci
October 2024
Department of Chemistry, Adam Mickiewicz University, Uniwersytetu Poznanskiego 8, 61-614 Poznan, Poland.
The antiproliferative and antibacterial activities of thiosemicarbazones increase markedly with the presence of metal ions. One of the factors determining the activity of metal thiosemicarbazone complexes is the coordination structure. In this study, the biological effects of new antimony (III) and bismuth (III) thiosemicarbazone complexes with different binding modes and geometrical structures were demonstrated.
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