Mulyana, Fathoni Ega and Waskitha, Stephanus Satria Wira and Pranowo, Deni and Khairuddean, Melati and Wahyumingsih, Tutik Dwi (2023) Synthesis of chalcone derivatives with methoxybenzene and pyridine moieties as potential antimalarial agents. Pharmacia, 70 (4). 1305 – 1313. ISSN 04280296
Full text not available from this repository.Abstract
Malaria remains an endemic disease in tropical regions, urgently needed the search for effective antimalarial agents due to resistance against existing drugs. This study investigated the potential antimalarial activity of pyridine-based chalcone derivatives against P. falciparum 3D7 and FCR3 strains. The chalcones were synthesized through a one-pot method using various pyridine carbaldehyde, resulting in yields ranging from 53.74 to 86.37, and all products were characterized using FTIR, GC-MS, and NMR spectroscopies. Among the six chalcones tested, chalcone A 1-(2-methoxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one displayed the highest antimalarial activity with IC50 values of 0.48 and 0.31 μg/mL against P. falciparum 3D7 and FCR3 strains, respectively, and a resistance index of 0.65. Molecular docking studies highlighted the interaction of the carbonyl group of all chalcones with Asn108 amino acid residue in the PfDHFR-TS active site via hydrogen bonding, demonstrating their potential as the antimalarial agent. Notably, the positioning of methoxy and pyridine substituents significantly influenced the antimalarial activity of the chalcones. © Mulyana FE et al. This is an open access article distributed under the terms of the Creative Commons Attribution License (CC-BY 4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Item Type: | Article |
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Additional Information: | Cited by: 0; All Open Access, Gold Open Access |
Uncontrolled Keywords: | amino acid; anisole; carbonyl derivative; chalcone c; chalcone d; chalcone derivative; chalcone e; chalcone f; chloroquine; licochalcone A; licochalcone B; ligand; pyridine; pyridine derivative; unclassified drug; antimalarial activity; Article; carbon nuclear magnetic resonance; controlled study; drug synthesis; Fourier transform infrared spectroscopy; human; hydrogen bond; IC50; in vitro study; malaria; mass fragmentography; molecular docking; molecular interaction; nonhuman; nuclear magnetic resonance; nuclear magnetic resonance spectroscopy; Plasmodium falciparum; Plasmodium falciparum 3D7; Plasmodium falciparum FCR3; proton nuclear magnetic resonance; thin layer chromatography |
Subjects: | R Medicine > RB Biomedical Sciences |
Divisions: | Faculty of Medicine, Public Health and Nursing > Biomedical Sciences |
Depositing User: | Sri JUNANDI |
Date Deposited: | 30 Oct 2024 01:21 |
Last Modified: | 30 Oct 2024 01:21 |
URI: | https://ir.lib.ugm.ac.id/id/eprint/6002 |