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四氢-β-咔啉衍生物的合成与植物病原真菌抑制剂的研究。

Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of Plant Pathogenic Fungi.

机构信息

Department of Chemistry, Faculty of Science, Silpakorn University, Nakhon Pathom 73000, Thailand.

Department of Science, Faculty of Liberal Arts and Science, Kamphaeng Sean Campus, Kasetsart University, Nakhon Pathom 73140, Thailand.

出版信息

Molecules. 2021 Jan 3;26(1):207. doi: 10.3390/molecules26010207.

DOI:10.3390/molecules26010207
PMID:33401587
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7796172/
Abstract

A series of tetrahydro-ß-carbolines substituted with an alkyl or acyl side chain was synthesized and screened for its antifungal activity plant pathogenic fungi (, , and ). The structure activity relationship revealed that the substituent at the piperidine nitrogen plays an important role for increasing antifungal activities. In this series, 2-octyl-2,3,4,9-tetrahydro-1-pyrido[3,4-]indole () displayed potent antifungal activities with a minimum inhibitory concentration of 0.1 μg/mL, including good inhibitory activity to the radial growth of fungus at a concentration of 100 μg/mL compared to amphotericin B.

摘要

一系列具有烷基或酰基侧链的四氢-β-咔啉被合成并筛选其对植物病原真菌(、、和)的抗真菌活性。构效关系表明,哌啶氮上的取代基对于提高抗真菌活性起着重要作用。在这个系列中,2-辛基-2,3,4,9-四氢-1-吡啶并[3,4-]吲哚()表现出很强的抗真菌活性,最低抑菌浓度为 0.1μg/mL,与两性霉素 B 相比,在 100μg/mL 的浓度下对真菌的径向生长也有很好的抑制活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/d2d30d6f2c2f/molecules-26-00207-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/9b79098238ea/molecules-26-00207-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/06e57e59721c/molecules-26-00207-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/d2d30d6f2c2f/molecules-26-00207-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/9b79098238ea/molecules-26-00207-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/06e57e59721c/molecules-26-00207-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/966c/7796172/d2d30d6f2c2f/molecules-26-00207-g002.jpg

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