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3,4-Dihydropyrimidinone-coumarin analogues as a new class of selective agent against S. aureus: Synthesis, biological
Nirmala S Naik1, Lokesh A Shastri1, Shrinivas D Joshi2
1Department of Chemistry, Karnatak University, Dharwad 580 003, Karnataka, India.
Abstract:
Bacterial infections are increasingly difficult to combat as bacteria evolve resistance to antibiotic drugs and have severely compromised the arsenal of antibiotic drugs. On the other hand matrix metalloproteinases (MMPs) play a fundamental role in inflammation and extracellular matrix degradation in physiological and pathological conditions. In search of potent antibiotic, taking coumarin and dihydropyrimidinone as lead compound, a green, eco-friendly and efficient protocol has been developed and synthesized the dihydropyrimidin-2(1H)-one/thione derivatives of coumarin 3/4 from substituted 4-formylcoumarins 2 and ethylacetoacetate using urea/thiourea in the presence of catalytic amount of ceric ammonium nitrate is reported. All the synthesized compounds were evaluated for their antibacterial activity against four bacterial strains by broth dilution method. The tested compounds have exhibited promising in vitro potency with low MIC values against the drug susceptive S. aureus strain with low MIC values ranging from 0.2 to 6.25μg/mL. The in vivo anti-inflammatory potency of 3a-e and 4a-e by gelatin zymography is comparable to that of tetracycline. Molecular docking study performed for all the synthesized compounds with S. aureus DNA gyrase and results obtained were quite promising.
Insights
New coumarin and dihydropyrimidinone derivatives show potent antibacterial and anti-inflammatory activity. These compounds offer promising potential against drug-resistant bacteria and inflammation, with promising molecular docking results.
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Pharmacology
Background:
- Antibiotic resistance is a growing global health threat, necessitating novel drug discovery.
- Matrix metalloproteinases (MMPs) are key targets for anti-inflammatory drug development.
Purpose of the Study:
- To synthesize novel coumarin-dihydropyrimidinone derivatives as potential antibiotics and anti-inflammatory agents.
- To evaluate the antibacterial and anti-inflammatory efficacy of the synthesized compounds.
Main Methods:
- Green synthesis of dihydropyrimidin-2(1H)-one/thione derivatives from substituted 4-formylcoumarins.
- Broth dilution method for in vitro antibacterial activity assessment.
- Gelatin zymography for in vivo anti-inflammatory evaluation and molecular docking with S. aureus DNA gyrase.
Main Results:
- Synthesized compounds demonstrated significant in vitro antibacterial activity against S. aureus, with MIC values as low as 0.2 μg/mL.
- In vivo anti-inflammatory potency was comparable to tetracycline.
- Molecular docking studies indicated promising interactions with S. aureus DNA gyrase.
Conclusions:
- The novel coumarin-dihydropyrimidinone derivatives exhibit potent antibacterial and anti-inflammatory properties.
- These compounds represent promising candidates for further development against bacterial infections and inflammatory conditions.
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