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脂肪族和芳香族内酯的杀利什曼原虫活性：构效关系

Leishmanicidal activity of aliphatic and aromatic lactones: correlation structure-activity.

作者信息

Castaño Marcela, Cardona Wilson, Quiñones Winston, Robledo Sara, Echeverri Fernando

机构信息

Grupo de Química Orgánica de Productos Naturales-SIU, Universidad de Antioquia, P.O. Box 1226, Medellín, Colombia.

出版信息

Molecules. 2009 Jul 10;14(7):2491-500. doi: 10.3390/molecules14072491.

DOI:10.3390/molecules14072491
PMID:19633618
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6255270/
Abstract

Several aliphatic and aromatic lactones and two dimers were synthesized using the sequence: allylation - esterification - metathesis. These compounds were active in vitro against intracellular amastigotes of Leishmania panamensis. The structure-activity relationship showed the importance of the aliphatic side chain to enhance the biological activity and to obtain lower cytotoxicity. It was also observed that a decrease in the size of the lactone ring increases the selectivity index.

摘要

使用烯丙基化-酯化-复分解反应序列合成了几种脂肪族和芳香族内酯以及两种二聚体。这些化合物在体外对巴拿马利什曼原虫的细胞内无鞭毛体具有活性。构效关系表明脂肪族侧链对于增强生物活性和获得较低细胞毒性的重要性。还观察到内酯环尺寸的减小会增加选择性指数。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/6fdaa028fd20/molecules-14-02491-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/9de2b4d3c00b/molecules-14-02491-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/ff0a5ba16634/molecules-14-02491-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/052016d79360/molecules-14-02491-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/6fdaa028fd20/molecules-14-02491-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/9de2b4d3c00b/molecules-14-02491-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/ff0a5ba16634/molecules-14-02491-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/052016d79360/molecules-14-02491-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a4cd/6255270/6fdaa028fd20/molecules-14-02491-g002.jpg

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