卡波烯衍生物的合成与抗真菌活性。

Synthesis and antifungal activity of carabrone derivatives.

机构信息

Research and Development Center of Biorational Pesticide, College of Plant Protection, Northwest A&F University, Yangling, China.

出版信息

Molecules. 2010 Sep 16;15(9):6485-92. doi: 10.3390/molecules15096485.

DOI:10.3390/molecules15096485

PMID:20877238

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6257742/

Abstract

Nine derivatives 6-14 of carabrone (1) were synthesized and tested in vitro against Colletotrichum lagenarium Ell et Halst using the spore germination method. Among all of the derivatives, compounds 6-8 and 12 showed more potent antifungal activity than 1. Structure-activity relationships (SAR) demonstrated that the γ-lactone was necessary for the antifungal activity of 1, and the substituents on the C-4 position of 1 could significantly affect the antifungal activity.

摘要

合成了 1 种 carabrone（1）的 9 种衍生物 6-14，并采用孢子萌发法对其进行了离体抗 Colletotrichum lagenarium Ell et Halst 的活性测试。在所有的衍生物中，化合物 6-8 和 12 比 1 表现出更强的抗真菌活性。构效关系（SAR）表明，γ-内酯对于 1 的抗真菌活性是必需的，并且 1 的 C-4 位取代基可以显著影响其抗真菌活性。