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Volume 18, Issue 3
  • ISSN: 2212-7968
  • E-ISSN: 1872-3136

Abstract

Background

Chalcones have been demonstrated to possess numerous therapeutic qualities in recent years, such as antibacterial, antiviral, anti-ulcerative, antioxidant, anti-inflammatory, antihyperglycemic, antimalarial, antitubercular, analgesic, antiplatelet, and anticancer activities.

Objective

To explore the synthesis, docking, and therapeutic characteristics of chalcones as antibacterial and anthelmintic compounds.

Methods

The chalcone derivatives (3a-3k) and (6l-6v) were synthesized two selective different reactions, based on the Claisen-Schmidt reaction. All synthesized compounds were evaluated for their antibacterial activity using an cup-plate method, and their anthelmintic activity was assessed using an earthworm paralysis and death assay. To validate these findings, conducted molecular docking experiments between the dihydrofolate reductase receptor (PDB ID: 4LAE) and the synthesised compounds (3a-3k) and (6l-6v) to determine catalytic interactions.

Results

Compound 6(n) exhibited the greatest efficacy in biological activity against compared to all other compounds examined. Compound 6(o) exhibited substantial efficacy against and . Emphasizing these findings, the compounds 3(a), 3(g), 3(i), 6(n), and 6(o) demonstrated hydrogen bond interactions with certain amino acid residues of the receptor, including THR 122, ASN 18, ASN19, GLN 96, SER 50, and ALA 8, during molecular docking.

Conclusion

The study results showed that the synthesised derivative 6(n) had beneficial antibacterial properties against , while derivative 6(o) exhibited antibacterial activity against and anthlelmintic activity against .

© 2024 Bentham Science Publishers
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2024-10-18
2025-05-07

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Synthesis, Docking Analysis, and Assessment of Chalcones for Antibacterial and Anthelmintic Activities
Curr Chem Biol 18, 176 (2024); https://doi.org/10.2174/0122127968347168241015102108
/content/journals/ccb/10.2174/0122127968347168241015102108
/content/journals/ccb/10.2174/0122127968347168241015102108
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  • Article Type:     Research Article
Keyword(s): 1-(naphthalen-2-yl)ethanone; 1-phenylethanone; anthelmintics; antibacterials; Chalcones; DHFR receptor; E. coli; molecular docking

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