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Antifungal activity of aminoalcohols and diamines against dermatophytes and yeast
Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2020-09-23 , DOI: 10.1007/s00044-020-02636-y
César A. Caneschi , Bruno A. de Oliveira , Angelina M. de Almeida , Renata P. do Carmo , Francislene J. Martins , Mauro V. de Almeida , Nádia R. B. Raposo

Dermatomycoses are infections caused by fungi and yeasts and the drug treatment is considered expensive and extensive. Researchers are synthesizing new organic compounds in order to obtain more effective molecules that provide reduced adverse effects. Our research group has synthesized and evaluated the biological activities of aminoalcohol and diamine derivatives, which were considered active against human pathogenic fungi. Therefore, the objective of this study was to evaluate the in vitro antifungal activity of aminoalcohols and diamine derivatives against fungi and yeasts that cause dermatomycoses. The minimum inhibitory concentrations (MICs) and the minimum fungicidal concentration (MFC) of aminoalcohol (1–4) and diamine (5–13) derivatives was determined against Trichophyton mentagrophytes, T. rubrum, Epidermophyton floccosum, and Candida albicans according to protocols from the Clinical and Laboratory Standards Institute. All molecules exhibited fungicidal activity against the evaluated fungal strains, with the MIC and MFC ranging between 0.12 and 1000 μg/mL for filamentous fungi and 0.6 and 1250 μg/mL for yeasts. The best activity was attributed to diamines compared to aminoalcohols, with an emphasis on molecules 6 and 7. These results demonstrate the antifungal potential of the evaluated aminoalcohols and diamines against the four primary fungal species that cause dermatomycoses.



中文翻译:

氨基醇和二胺类对皮肤真菌和酵母菌的抗真菌活性

皮肤粘膜病是由真菌和酵母菌引起的感染,药物治疗被认为是昂贵且广泛的。研究人员正在合成新的有机化合物,以获得更有效的分子,从而减少不良影响。我们的研究小组已经合成并评估了氨基醇和二胺衍生物的生物活性,它们被认为对人类病原性真菌具有活性。因此,本研究的目的是评估氨基醇和二胺衍生物对引起皮肤真菌病的真菌和酵母菌的体外抗真菌活性。测定了氨基醇(1-4)和二胺(5-13)衍生物的最小抑制浓度(MIC)和最小杀真菌浓度(MFC)。根据临床和实验室标准协会的规程,毛癣菌红毛癣菌絮状表皮白色念珠菌。所有分子均显示出对所评价真菌菌株的杀真菌活性,其中丝状真菌的MIC和MFC范围为0.12至1000μg/ mL,酵母菌的MIC和MFC范围为0.6至1250μg/ mL。最好的活性归因于二胺相比氨基醇,与分子的强调小号6个7这些结果表明所评估的氨基醇与二胺靠在四个主要的真菌物种引起皮肤真菌病的抗真菌潜力。

更新日期:2020-10-07
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