Lima Tamires C, Ferreira Alana R, Silva Daniele F, Lima Edeltrudes O, de Sousa Damião P
a Department of Pharmacy , Federal University of Sergipe , São Cristóvão , Brazil.
b Department of Pharmaceutical Sciences , Federal University of Paraíba , João Pessoa , Brazil.
Nat Prod Res. 2018 Mar;32(5):572-575. doi: 10.1080/14786419.2017.1317776. Epub 2017 Apr 20.
Candida albicans is an important opportunistic fungal pathogen capable of provoking infection in humans. In the present study, we evaluated the antifungal effect of 23 ester derivatives of the cinnamic and benzoic acids against 3 C. albicans strains (ATCC-76645, LM-106 and LM-23), as well as discuss their Structure-Activity Relationship (SAR). The antifungal assay results revealed that the screened compounds exhibited different levels of activity depending on structural variation. Among the ester analogues, methyl caffeate (5) and methyl 2-nitrocinnamate (10) were the analogues that presented the best antifungal effect against all C. albicans strains, presenting the same MIC values (MIC = 128 μg/mL), followed by methyl biphenyl-2-carboxylate (21) (MIC = 128, 128 and 256 μg/mL for C. albicans LM-106, LM-23, and ATCC-76645, respectively). Our results suggest that certain molecular characteristics are important for the antifungal action.
白色念珠菌是一种重要的机会性真菌病原体，能够引发人类感染。在本研究中，我们评估了23种肉桂酸和苯甲酸酯衍生物对3株白色念珠菌（ATCC - 76645、LM - 106和LM - 23）的抗真菌作用，并讨论了它们的构效关系（SAR）。抗真菌试验结果表明，所筛选的化合物根据结构变化表现出不同程度的活性。在酯类似物中，咖啡酸甲酯（5）和2 - 硝基肉桂酸甲酯（10）是对所有白色念珠菌菌株表现出最佳抗真菌效果的类似物，呈现相同的最低抑菌浓度值（MIC = 128μg/mL），其次是联苯 - 2 - 羧酸甲酯（21）（对白色念珠菌LM - 106、LM - 23和ATCC - 76645的MIC分别为128、128和256μg/mL）。我们的结果表明，某些分子特征对抗真菌作用很重要。
