The Key Laboratory of Miao Medicine of Guizhou Province, School of Pharmacy, Guizhou University of Traditional Chinese Medicine, Guiyang 550025, China.
School of Chinese Medicine, Hong Kong Baptist University, Hong Kong 999077, China.
Molecules. 2022 Oct 12;27(20):6836. doi: 10.3390/molecules27206836.
In order to discover more promising antifungal and antibacterial agents, a series of new derivatives were designed and synthesized by structure modification based on the naturally occurring antimicrobial compound lophanic acid. The structures of all the target compounds were well characterized by spectroscopic data. The stereochemistry of these compounds was further determined through the X-ray diffraction analysis of 6a. The synthetic compounds were evaluated for their antimicrobial activities against filamentous fungi (), yeasts () and Gram-positive and Gram-negative bacteria ( and ). Among them, 3d and 3i are found as the most promising leads that showed potent inhibitory effects against all the tested fungal and bacterial strains except for . The presence of the C-20 carboxylic ester groups and the free hydroxy group at C-13 was found to be essential for the antifungal and antibacterial activities of the lophanic acid derivatives.
为了发现更有前途的抗真菌和抗菌剂，我们基于天然存在的抗菌化合物洛伐那酸进行了结构修饰，设计并合成了一系列新的衍生物。所有目标化合物的结构均通过光谱数据得到了很好的表征。通过对 6a 的 X 射线衍射分析进一步确定了这些化合物的立体化学。对合成化合物进行了抗丝状真菌（）、酵母（）和革兰氏阳性和革兰氏阴性细菌（和）的抗菌活性评价。其中，3d 和 3i 被发现是最有前途的先导化合物，它们对所有测试的真菌和细菌菌株都显示出强大的抑制作用，除了。洛伐那酸衍生物的抗真菌和抗菌活性，需要 C-20 羧酸酯基团和 C-13 上的游离羟基的存在。
