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.
Highlights
Pyrazole and pyrazolone motifs are well known for their wide range of biological activities such as antimicrobial, anti-inflammatory, and antitumor activities
Understanding that the incorporation of both pyrazole and pyrazolone together in the same scaffold could provide novel compounds with interesting biological activities coupled with our continuing research interest in the field of 4functionalized pyrazole derivatives [12,21-23] and other biologically active synthetic heterocyclic compounds [24-27], we set out to undertake the synthesis of some novel 4-arylidene pyrazole derivatives bearing benzenesulfonamide moiety at the N1-position of the pyrazole ring (Scheme 1) as potential antimicrobial agents
In conclusion, we have presented the novel 4-arylidene pyrazole derivatives bearing benzenesulfonamide moiety as potential antimicrobial agents
Summary
Pyrazole and pyrazolone motifs are well known for their wide range of biological activities such as antimicrobial, anti-inflammatory, and antitumor activities. Pyrazol-5-(4H)-one constitutes the core scaffold of various biologically active synthetic heterocyclic compounds which have been associated with some interesting pharmaceutical properties, including analgesic [15], antimicrobial [16,17], anti-inflammatory [18], antitumor [19], and cytotoxicity [20] properties. Understanding that the incorporation of both pyrazole and pyrazolone together in the same scaffold could provide novel compounds with interesting biological activities coupled with our continuing research interest in the field of 4functionalized pyrazole derivatives [12,21-23] and other biologically active synthetic heterocyclic compounds [24-27], we set out to undertake the synthesis of some novel 4-arylidene pyrazole derivatives bearing benzenesulfonamide moiety at the N1-position of the pyrazole ring (Scheme 1) as potential antimicrobial agents
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