Synthesis and biological evaluation of pyrazolo[1,5-a]pyrimidine-3-carboxamide as antimicrobial agents
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Exploring novel classes of antimicrobial therapeutics is an excellent approach to face the challenge of microbial resistance. In this context, a novel series of pyrazolo[1,5-a]pyrimidines 5a–d, 10a–f, 15a, d and 16a–d were synthesized and characterized by their spectral data. The structure of 10f was confirmed by X-ray diffraction analysis of its single crystal. The antimicrobial activities of the newly synthesized compounds showed that, compounds 5a and 16d were more potent than tetracycline against Bacillus subtilis, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. In addition, most of the newly synthesized compounds displayed a significant antifungal activity when compared with amphotericin B. Moreover, compound 16d (27.0 ± 0.41 mm, minimum inhibitory concentration: 7.81 µg/ml) displayed excellent and the highest antifungal activity than amphotericin B (18.0 ± 0.17 mm, MIC: 15.62 µg/ml) against Fusarium oxysporum.
Keywords5-Aminopyrazole Pyrazolo[1,5-a]pyrimidine Antimicrobial agents X-ray crystallography
The authors wish to express their thanks to the National Research Centre for the facilities provided. Farid Sroor is grateful to the embassy of France in Cairo for a postdoctoral scholarship within the Institut Fancais d' Egypte (IFE) program and he thankful to Prof. Michel Etienne and Laure Vendier at the LCC for their support in the analysis.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no competing interests.
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