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Multifunctional Curcumin-Inspired 3,5-Diarylidene-4-Piperidones: Design, Synthesis, Biological Evaluation and
Angel K Nkosi1, Adel S Girgis2, Ahmed Samir3
1Department of Chemistry and Biochemistry, Augusta University, Augusta, GA 30912, USA.
Pharmaceuticals (Basel, Switzerland)
|June 26, 2026
Summary
New curcumin-inspired piperidones show potent antibacterial activity against Staphylococcus aureus, inhibiting biofilm formation and DNA gyrase. These multifunctional compounds offer a promising platform for developing novel antibacterial agents.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Antimicrobial Research
Background:
- Antimicrobial resistance necessitates novel chemotypes with diverse mechanisms.
- Curcumin derivatives offer a scaffold for developing multifunctional antibacterial agents.
Purpose of the Study:
- Design, synthesize, and evaluate curcumin-inspired 3,5-diarylidene-4-piperidones.
- Assess antibacterial, antibiofilm, anti-efflux, DNA gyrase-inhibitory, and antiproliferative properties.
Main Methods:
- Copper-catalyzed click chemistry for synthesis.
- Antibacterial assays against Gram-positive and Gram-negative bacteria.
- DNA gyrase inhibition, antibiofilm, anti-efflux, and antiproliferative evaluations.
- QSAR and molecular docking for mechanistic insights.
Main Results:
- Selective activity against Gram-positive bacteria, especially Staphylococcus aureus.
- Compounds 7n and 7l showed potent anti-S. aureus activity (MICs 7.8 and 8.2 μM).
- Compound 7l inhibited S. aureus DNA gyrase (IC50 3.20 μM); compound 7e showed strong antibiofilm activity; compound 7a demonstrated anti-efflux properties.
Conclusions:
- Triazole-conjugated 3,5-diarylidene-4-piperidones are effective multifunctional antibacterial scaffolds.
- Compound 7l exhibits potent DNA gyrase inhibition, offering a lead for new antibacterial drug development.
- This chemotype shows potential for developing polymechanistic antibacterial agents.
Keywords:
4-piperidonesStaphylococcus aureusantimicrobialbiofilmcancerefflux pumpgyrasemolecular modelingMore Related Videos
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