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Molecules 2014, 19(5), 5806-5820; doi:10.3390/molecules19055806

Anti-Candida, Anti-Enzyme Activity and Cytotoxicity of 3,5-Diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides

1,* , 5
1 Laboratory of Microbiology, Postgraduate Program in Dentistry, School of Dentistry, Federal University of Pelotas (UFPel)—Rua Gonçalves Chaves, 457/504, Pelotas, RS 96015-000, Brazil 2 Faculty of Exact Sciences and Technology, Federal University of Grande Dourados, Dourados, MS 79825-070, Brazil 3 Department of Chemistry and the Consortium for Photochemical Technology (NAP-PhotoTech), University of São Paulo, São Paulo, SP 05508-000, Brazil 4 School of Chemistry and Food, Federal University of Rio Grande, Rio Grande, RS 95500-000, Brazil 5 Laboratory of Bioactive Heterocycles and Bioprospection (LAHBBio), Center for Chemical, Pharmaceutical and Food Sciences, Federal University of Pelotas, Pelotas, RS 96010-610, Brazil 6 Department of Restorative Dentistry, School of Dentistry, Federal University of Pelotas (UFPel), Pelotas, RS 96015-000, Brazil
* Author to whom correspondence should be addressed.
Received: 6 February 2014 / Revised: 14 April 2014 / Accepted: 16 April 2014 / Published: 6 May 2014
(This article belongs to the Section Organic Synthesis)
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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 were (p = 0.01), and 15.6 μg/mL was the most effective concentration. The cytotoxicity means were similar among the tests (p = 0.32). These compounds could be useful as templates for further development through modification or derivatization to design more potent antifungal agents. Data from this study provide evidence that these new pyrazole formulations could be an alternative source for the treatment of fungal infections caused by Candida. However, a specific study on the safety and efficacy of these in vivo and clinical trials is still needed, in order to evaluate the practical relevance of the in vitro results.
Keywords: pyrazoles; Candida albicans; antifungal activity; anti-enzyme activity pyrazoles; Candida albicans; antifungal activity; anti-enzyme activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Oliveira, S.; Pizzuti, L.; Quina, F.; Flores, A.; Lund, R.; Lencina, C.; Pacheco, B.S.; de Pereira, C.M.P.; Piva, E. Anti-Candida, Anti-Enzyme Activity and Cytotoxicity of 3,5-Diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides. Molecules 2014, 19, 5806-5820.

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