Unlocking the Biological Potential of 2-Pyridones: Synthesis, Antioxidant and Antimicrobial Activity of N-Phenacylated 5/6-Chloro-2-pyridones.

Sarita Sangwan, Sonu Chauhan, Neelam Yadav, Ravi Kumar, Anil Duhan, Vinod Malik, Jayant Sindhu

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Article in Medicinal chemistry (Shariqah (United Arab Emirates)), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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Sarita SangwanDepartment of Chemistry, College of Basic Sciences and Humanities, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.ORCID 0000-0001-8413-1478

Sonu ChauhanDepartment of Chemistry, College of Basic Sciences and Humanities, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.

Neelam YadavDepartment of Chemistry, College of Basic Sciences and Humanities, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.ORCID 0000-0003-1159-0969

Ravi KumarDepartment of Chemistry, College of Basic Sciences and Humanities, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.ORCID 0000-0001-8146-9799

Anil DuhanDepartment of Chemistry, College of Basic Sciences and Humanities, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.ORCID 0009-0003-5249-2668

Vinod MalikDepartment of Plant Pathology, College of Agriculture, Chaudhary Charan Singh Haryana Agricultural University, Haryana, Hisar, 125004, India.

Jayant SindhuDepartment of Chemistry, CCS HAU Hisar Haryana, 125004, India.

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6 · The paper itself

Abstract

aimsA simple and efficient synthesis of 14 new (9a-9n) N-phenacyl-2-pyridones with good yields (up to 75%), is reported. The synthesized derivatives were screened for their in vitro radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH), their in vitro antimicrobial potential was tested against human pathogenic bacterial strains, including

methodsAll compounds displayed modest antioxidant activity, with compound 9b being the most potent in the DPPH radical scavenging assay. Most of the synthesized compounds exhibited good to excellent antimicrobial activity, however, the compounds (9d, and 9b) showed maximum inhibition zone diameters of 18.75, and 18.25 mm respectively, demonstrating better antimicrobial potential than the standard drug streptomycin against

resultsCompound 9f was found most effective against

conclusionThe electron-withdrawing substituents on the aryl ring of synthesized N-phenacyl-2- pyridones improved the antioxidant activity, however, for Gram-positive bacteria, less lipophilic or more hydrophilic substituents, such as halogens, displayed better antimicrobial activity. Similarly, it was the more lipophilic substitutions on the aryl ring that improved the antimicrobial activity against Gram-negative bacteria.

Indexed as

Anti-Bacterial AgentsAntifungal AgentsAnti-Infective AgentsAntioxidantsPyridonesBiphenyl CompoundsCandida albicansEscherichia coliMicrobial Sensitivity TestsMolecular Docking SimulationMolecular StructurePicratesPseudomonas aeruginosaStaphylococcus aureusStructure-Activity Relationship1,1-diphenyl-2-picrylhydrazylAnti-Bacterial AgentsAntifungal AgentsAnti-Infective AgentsAntioxidantsBiphenyl CompoundsPicratesPyridones2-Pyridonesantibacterial activityantioxidant activitynitrogen heterocyclesN-phenacylationSAR study

Identifiers

PMID39950275

DOI10.1016/j.ejmech.2011.08.049

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