Serious fungal infections are increasing worldwide and have become a great concern in the medical field since antifungal drugs are restricted to a few drug classes. This work aims to evaluate the antifungal activity of a series of 5-amino-1-aryl-3-methyl-1H-pyrazole-4-carbonitriles (1a-g) and to establish a structure-activity relationship (SAR). The synthesis of these compounds was carried out in a single step followed by cyclization in good to excellent yields i.e. 73-94%. The chemical structures were confirmed by melting point, IR, 1H-NMR, 13C-NMR, and HRMS. These seven compounds were submitted to the disk diffusion test against Candida spp. and the active compound was evaluated by means of the microdilution method to determine the minimum inhibitory concentration (MIC). In addition, the stereo electronic descriptors were evaluated and pharmacokinetic and toxicological properties were calculated to predict the potential of these compounds as a drug. All the compounds presented good theoretical physicochemical parameters and one of them showed reasonably good antifungal activity.

由于抗真菌药物仅限于几种药物类别，因此严重的真菌感染在全球范围内正在增加，并已成为医学领域的重大关注。这项工作旨在评估一系列的5-氨基-1-芳基-3-甲基-1H-吡唑-4-腈（1a-g）的抗真菌活性，并建立结构-活性关系（SAR）。这些化合物的合成是一步完成的，然后以良好至极好的收率（即73-94％）环化。通过熔点，IR，1 H-NMR，13 C-NMR和HRMS确认化学结构。这七个化合物已针对假丝酵母菌进行了圆盘扩散测试。并通过微量稀释法评估活性化合物，以确定最小抑菌浓度（MIC）。此外，评估了立体电子描述符，并计算了药代动力学和毒理学特性，以预测这些化合物作为药物的潜力。所有化合物均具有良好的理论理化参数，其中之一具有相当好的抗真菌活性。