Synthesis and Evaluation of the Fungal Activity of New Pyrazole-Carboxamides Against Colletotrichum gloeosporioides (original) (raw)
2020, Journal of the Brazilian Chemical Society
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Series of seven 5-phenyl-1H-pyrazole-3-carboxylic acid amide derivatives were prepared by varying the active part (amide group) of pyrazole. All the synthesized compounds were characterized by, H NMR, C NMR and mass spectrometry and were screened, antifungal activity, against four fungal pathogens such as Candida albicans, Aspergillus flavus, Aspergillus fumigatus and Aspergillus niger using broth microdilution method. Active compounds were also screened for MIC (minimum inhibitory concentration) and MFC (minimum fungicidal concentrations). Two compounds 5b and 5f were found to be more potent than standard actidione drugs, against Candida albicans strains.
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Because of the need for more effective and less harmful antifungal therapies, and interest in the synthesis of new carboximidamides, the goal of this study was to determine the antifungal and anti-enzyme activities of some new pyrazole carboximidamides and their cytotoxicity. For this purpose, tests were performed to evaluate: minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC); production of proteinases and phospholipase, and cytotoxicity of the extracts. Data were analyzed by ANOVA and Tukey Tests (α = 5%). The results were: MIC and MFC ≥ 62.5 μg/mL (C. albicans, C. parapsilosis, C. famata, C. glabrata, and Rhodotorula mucillaginosa) and MIC and MFC ≥ 15.6 μg/mL (C. lipolytica). The values of proteinase and phospholipase (Pz) of C. albicans before and after exposure to the compounds were: 0.6 (±0.024) and 0.2 (±0.022) and 0.9 (±0.074) and 0.3 (±0.04), respectively. These proteinase results were not significant (p = 0.69), but those of phospholipase we...
A novel series of Carboxamide derivative of N-(3-fluoro-4-morpholinophenyl)-3-methyl-5-(methylthio)-1H-pyrazole-4-carboxamide have been synthesized by using different aromatic acid chloride in very good yield. The structures of the synthesized compounds have been characterized by using IR, 1 H NMR and Mass spectroscopy. All the prepared new NCEs were screened for anti microbial activity and anti fungal activity.
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