ArticleOrganic and medicinal chemistry letters2013
Synthesis of some novel 4-arylidene pyrazoles as potential antimicrobial agents.
Article in Organic and medicinal chemistry letters, 2013. 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.
- GC Analysis, Anticancer, and Antibacterial Activities of Secondary Bioactive Compounds from Endosymbiotic Bacteria of Pomegranate Aphid and Its Predator and Protector.Molecules (Basel, Switzerland) · 2023Article
- New Potent 5α- Reductase and Aromatase Inhibitors Derived from 1,2,3-Triazole Derivative.Molecules (Basel, Switzerland) · 2020Article
- Synthesis and evaluation of novel spiro derivatives for pyrrolopyrimidines as anti-hyperglycemia promising compounds.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Crystal structure of ethyl 2-({[(4Z)-3,5-dioxo-1-phenyl-pyrazolidin-4-yl-idene]meth-yl}amino)-acetate.Acta crystallographica. Section E, Structure reports online · 2014Article
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Authors and funding
5 authors.
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Abstract
backgroundPyrazole and pyrazolone motifs are well known for their wide range of biological activities such as antimicrobial, anti-inflammatory, and antitumor activities. The incorporation of more than one pharmacophore in a single scaffold is a well known approach for the development of more potent drugs. In the present investigation, a series of differently substituted 4-arylidene pyrazole derivatives bearing pyrazole and pyrazolone pharmacophores in a single scaffold was synthesized.
resultsThe synthesis of novel 4-arylidene pyrazole compounds is achieved through Knovenagel condensation between 1,3-diaryl-4-formylpyrazoles and 3-methyl-1-phenyl-1H-pyrazol-5-(4H)-ones in good yields. All compounds were evaluated for their in vitro antimicrobial activity.
conclusionsA series of 4-arylidene pyrazole derivatives was evaluated for their in vitro antimicrobial activity against two Gram-positive (Bacillus subtilis and Staphylococcus aureus) and two Gram-negative bacteria (Pseudomonas fluorescens and Escherichia coli), as well as two pathogenic fungal strains (Candida albicans and Saccharomyces cerevisiae). The majority of the compounds displayed excellent antimicrobial profile against the Gram-positive (B. subtilis and S. aureus), and some of them are even more potent than the reference drug ciprofloxacin.
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