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雏菊中聚乙炔类化合物及其合成衍生物的抗菌活性

Antimicrobial activity of polyacetylenes from Bellis perennis and their synthetic derivatives.

作者信息

Avato P, Vitali C, Mongelli P, Tava A

机构信息

Dipartimento Farmaco-Chimico, Facoltà di Farmacia, Università, Bari, Italy.

出版信息

Planta Med. 1997 Dec;63(6):503-7. doi: 10.1055/s-2006-957751.

DOI:10.1055/s-2006-957751
PMID:9434600
Abstract

The chemical investigation of the essential oils from the aerial organs of Bellis perennis L., the common daisy, showed that polyacetylenes were one of the dominant class of compounds. The major constituents, methyl deca-4,6-diynoate and deca-4,6-diynoic acid, and their structural analogues, deca-4,6-diyne, dimethyl octa-3,5-diyne-1,8-dioate and deca-4,6-diyne-1,10-dioic acid, were synthesised and their antimicrobial activity evaluated. Only deca-4,6-diynoic acid and deca-4,6-diyne-1,10-dioic acid showed antimicrobial activity, being the two compounds mainly effective against Gram-positive and Gram-negative bacteria, respectively. Structure-activity relationships of the tested polyacetylenes are discussed.

摘要

对普通雏菊(Bellis perennis L.)地上部分的精油进行化学研究表明,聚乙炔是主要的化合物类别之一。合成了主要成分癸-4,6-二炔酸甲酯和癸-4,6-二炔酸及其结构类似物癸-4,6-二炔、二甲基辛-3,5-二炔-1,8-二酸酯和癸-4,6-二炔-1,10-二酸,并评估了它们的抗菌活性。只有癸-4,6-二炔酸和癸-4,6-二炔-1,10-二酸显示出抗菌活性,这两种化合物分别主要对革兰氏阳性菌和革兰氏阴性菌有效。讨论了所测试聚乙炔的构效关系。

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