ArticleMolecular diversity2024
Chrysin based pyrimidine-piperazine hybrids: design, synthesis, in vitro antimicrobial and in silico E. coli topoisomerase II DNA gyrase efficacy.
Article in Molecular diversity, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Comprehensive perspectives of metal and metal-free C-H activation approaches in pyrimidines and related heteroarenes: scope, mechanistic insights, and synthetic utility.RSC advances · 2025Review
- Chrysin as a Bioactive Scaffold: Advances in Synthesis and Pharmacological Evaluation.International journal of molecular sciences · 2025Review
- Epigenetic modulation of Ceratorhiza hydrophila by 5-azacytidine enhances antifungal metabolite production: insights from antimicrobial, metabolic, genomic and computational analyses.BMC microbiology · 2025Article
- Recent Advances in Pyrimidine-Based Drugs.Pharmaceuticals (Basel, Switzerland) · 2024Review
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Authors and funding
6 authors.
Funding
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Abstract
Ten chrysin-based pyrimidine-piperazine hybrids have been evaluated in vitro for antimicrobial activity against eleven bacterial and two fungal strains. All compounds 5a-j exhibited moderate to good inhibition, with MIC values ranging from 6.25 to 250 µg/ml. At 6.25 µg/ml and 12.5 µg/ml MIC values, respectively, compounds 5b and 5h demonstrated the most promising potency against E. coli, outperforming ampicillin, chloramphenicol, and ciprofloxacin. None of the substances had the same level of action as norfloxacin. 5a, 5d, 5g, 5h, and 5i have exhibited superior antifungal efficacy than Griseofulvin against C. albicans with 250 µg/ml MIC. All the compounds were also individually docked into the E. coli DNA gyrase ATP binding site (PDB ID: 1KZN) and CYP51 inhibitor (PDB ID: 5V5Z). The most active compound, 5h and 5g displayed a Glide docking score of - 5.97 kcal/mol and - 10.99 kcal/mol against DNA gyrase and 14α-demethylase enzyme CYP51 respectively. Potent compounds 5b, 5h, and 5g may be used to design new, innovative antimicrobial agents, according to in vitro, ADMET, and in silico biological efficacy analyses.
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Registered trials
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