Synthesis and biological evaluation of pyrazolo[1,5-a]pyrimidine-3-carboxamide as antimicrobial agents
| Autor: | Doaa M. Masoud, Ahmed A. Askar, Ashraf S. Hassan, Farid M. Sroor |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
biology
010405 organic chemistry medicine.drug_class Tetracycline Stereochemistry Chemistry Organic Chemistry Carboxamide Context (language use) Bacillus subtilis 010402 general chemistry biology.organism_classification Antimicrobial 01 natural sciences 0104 chemical sciences Minimum inhibitory concentration Amphotericin B Fusarium oxysporum medicine General Pharmacology Toxicology and Pharmaceutics medicine.drug |
| Zdroj: | Medicinal Chemistry Research. 26:2909-2919 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-017-1990-y |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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