Piperine is a natural alkaloid with a wide range of biological functions. Natural phenolic compounds existed in many essential oils (EOs) are plant-derived aroma compounds with broad range of biological activities, however, their actions are slow, and they are typically unstable to light or heat, difficult to extract and so on. In order to find high-potential fungicides derived from piperine, a series of piperine-directed essential oil derivatives were designed and synthesized. The structures of all molecules were confirmed by satisfied spectral data, including 1H NMR, 13C NMR and ESIMS. The target compounds were screened for their potential fungicidal activities against six species of plant pathogen fungi, including Rhizoctonia solani, Fusarium graminearum, Phomopsis adianticola, Alternaria tenuis Nees, Phytophthora capsici and Gloeosporium theae-sinensis. Some of target compounds exhibited moderate and broad-spectrum activity against tested fungi compared to the parental piperine. Further studies have shown that some different concentrations of compounds have significant inhibitory activity against Alternaria tenuis Nees and Phytophthora capsici compared to commercial carbendazim, and compound 2b exhibited particularly significant broad-spectrum fungicidal activity.

中文翻译：

---

基于胡椒碱支架的天然酚类衍生物作为潜在的抗真菌剂

胡椒碱是一种具有多种生物学功能的天然生物碱。许多香精油（EO）中存在的天然酚类化合物是植物来源的芳香化合物，具有广泛的生物活性，但是它们的作用很慢，并且通常对光或热不稳定，难以提取等。为了找到衍生自胡椒碱的高潜力杀真菌剂，设计并合成了一系列以胡椒碱为导向的精油衍生物。所有分子的结构均通过满意的光谱数据证实，包括1 H NMR，13 C NMR和ESIMS。筛选了目标化合物对六种植物病原真菌的潜在杀真菌活性，这些植物病原菌包括：茄丝枯萎病菌，禾谷镰刀菌，印度扁线菌，牛瘟链球菌，辣椒疫霉（Phytophthora capsici）和球孢（Geoeosporium theae-sinensis）。与亲本胡椒碱相比，一些目标化合物对被测真菌表现出中等和广谱的活性。进一步的研究表明，与市售多菌灵相比，一些不同浓度的化合物对tendaria tenuis Nees和Phytophthora capsici具有显着的抑制活性，化合物2b表现出特别显着的广谱杀真菌活性。