3 years ago

Synthesis and biological evaluation of pyrazolo[1,5- a ]pyrimidine-3-carboxamide as antimicrobial agents

Farid M. Sroor, Ashraf S. Hassan, Doaa M. Masoud, Ahmed A. Askar

Abstract

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 5ad, 10af, 15a, d and 16ad 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.

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-1990-y

DOI: 10.1007/s00044-017-1990-y

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