Journal
LATIN AMERICAN JOURNAL OF PHARMACY
Volume 41, Issue 3, Pages 660-665Publisher
COLEGIO FARMACEUTICOS PROVINCIA DE BUENOS AIRES
Keywords
antibacterial; antifungal; pyrazole; pyrazolidin-3-one; synthesis
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Funding
- Taif University, Taif, Saudi Arabia [TURSP-2020/80]
- Glocal University, Saharanpur, Uttar Pradesh, India
- Prince Sattam Bin Abdulaziz University, Al-Kharj, Kingdom of Saudi Arabia
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In this research, a series of pyrazole derivatives were synthesized and evaluated for their antimicrobial and antifungal activities. The results showed that some of the derivatives exhibited significant activity against various strains.
Pyrazole derivatives have attracted considerable attention because of their diverse chemotherapeutic potential. In the present research work, some 5-phenyl-4-(1H-pyrazol-1-yl)pyrazolidin-3-one derivatives (4a-f) were synthesized and evaluated for their in vitro antibacterial activities against Gram-positive Staphylococcus aureus, Bacillus subtilis, and Gram-negative Escherichia coli, Pseudomonas aeruginosa strains and antifungal activities against Aspergillus niger and Candida albicansstrains. The synthesized derivatives were characterized by infrared, nuclear magnetic resonance (H-1-NMR and C-13-NMR), and mass spectrometry. The result showed that the compounds 5-(4-methoxyphenyl)-4(1H-pyrazol-1-yl)pyrazolidin-3-one (4d), 5-(4-chlorophenyl)-4(1H-pyrazol-1-yl)pyrazolidin-3-one (4e), and 5-(4-nitrophenyl)-4-(1H-pyrazol-1-yl)pyrazolidin-3-one (4f) showed significant antimicrobial activities when compared to standard drugs (streptomycin as antibacterial drug and amphotericin-B as antifungal drug). Compound 4d was the most effective against both Gram-positive and Gram-negative bacteria while compounds 4e and 4f showed the most effective antifungal activity.
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