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醛类及相关化合物的抑制特性——一种新先导化合物的鉴定

Inhibitory Properties of Aldehydes and Related Compounds against -Identification of a New Lead.

作者信息

Mackrill John J, Kehoe Roberta A, Zheng Limian, McKee Mary L, O'Sullivan Elaine C, Prestwich Barbara M Doyle, McCarthy Florence O

机构信息

Department of Physiology, School of Medicine, University College Cork, T12 K8AF Cork, Ireland.

School of Chemistry and Analytical and Biological Chemistry Research Facility, University College Cork, Western Road, T12 K8AF Cork, Ireland.

出版信息

Pathogens. 2020 Jul 7;9(7):542. doi: 10.3390/pathogens9070542.

Abstract

The pathogen is responsible for catastrophic crop damage on a global scale which totals billions of euros annually. The discovery of new inhibitors of this organism is of paramount agricultural importance and of critical relevance to food security. Current strategies for crop treatment are inadequate with the emergence of resistant strains and problematic toxicity. Natural products such as cinnamaldehyde have been reported to have fungicidal properties and are the seed for many new discovery research programmes. We report a probe of the cinnamaldehyde framework to investigate the aldehyde subunit and its role in a subset of aromatic aldehydes in order to identify new lead compounds to act against . An ellipticine derivative which incorporates an aldehyde (9-formyl-6-methyl ellipticine, ) has been identified with exceptional activity versus with limited toxicity and potential for use as a fungicide.

摘要

这种病原体在全球范围内造成了灾难性的作物损害,每年总计达数十亿欧元。发现这种生物体的新抑制剂具有至关重要的农业意义,与粮食安全密切相关。随着耐药菌株的出现和毒性问题,目前的作物处理策略并不充分。据报道,肉桂醛等天然产物具有杀菌特性,是许多新发现研究项目的起点。我们报告了对肉桂醛骨架的一种探索,以研究醛亚基及其在一部分芳香醛中的作用,以便确定对抗……的新先导化合物。一种含有醛的椭圆玫瑰树碱衍生物(9-甲酰基-6-甲基椭圆玫瑰树碱)已被鉴定出对……具有卓越活性,毒性有限,有作为杀菌剂使用的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6951/7400633/3d4b046e9b08/pathogens-09-00542-g001.jpg

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