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Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives

A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi. Especially, compound F5 exhibited higher fungicidal activity against Rhizoctonia solani(53.3...

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Autores principales: Li, Zhibin, Chen, Shaohua, Zhu, Shaowen, Luo, Jianjun, Zhang, Yaomou, Weng, Qunfang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332272/
https://www.ncbi.nlm.nih.gov/pubmed/26263966
http://dx.doi.org/10.3390/molecules200813941
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author Li, Zhibin
Chen, Shaohua
Zhu, Shaowen
Luo, Jianjun
Zhang, Yaomou
Weng, Qunfang
author_facet Li, Zhibin
Chen, Shaohua
Zhu, Shaowen
Luo, Jianjun
Zhang, Yaomou
Weng, Qunfang
author_sort Li, Zhibin
collection PubMed
description A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi. Especially, compound F5 exhibited higher fungicidal activity against Rhizoctonia solani(53.35%) than commercial antiviral agent validamycin (36.4%); compound F16 exhibited high fungicidal activity against Oospora citriaurantii ex Persoon(43.28%). Some of the alkaloids and their derivatives (compounds F4 and F25) exhibited broad-spectrum fungicidal activity. Specifically, compound F4 exhibited excellent high broad-spectrum fungicidal activity in vitro, and the curative and protection activities against P. litchi in vivo reached 92.59% and 59.26%, respectively. The new derivative, F4, with optimized physicochemical properties, obviously exhibited higher activities both in vitro and in vivo; therefore, F4 may be used as a new lead structure for the development of fungicidal drugs.
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spelling pubmed-63322722019-01-24 Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives Li, Zhibin Chen, Shaohua Zhu, Shaowen Luo, Jianjun Zhang, Yaomou Weng, Qunfang Molecules Article A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi. Especially, compound F5 exhibited higher fungicidal activity against Rhizoctonia solani(53.35%) than commercial antiviral agent validamycin (36.4%); compound F16 exhibited high fungicidal activity against Oospora citriaurantii ex Persoon(43.28%). Some of the alkaloids and their derivatives (compounds F4 and F25) exhibited broad-spectrum fungicidal activity. Specifically, compound F4 exhibited excellent high broad-spectrum fungicidal activity in vitro, and the curative and protection activities against P. litchi in vivo reached 92.59% and 59.26%, respectively. The new derivative, F4, with optimized physicochemical properties, obviously exhibited higher activities both in vitro and in vivo; therefore, F4 may be used as a new lead structure for the development of fungicidal drugs. MDPI 2015-07-31 /pmc/articles/PMC6332272/ /pubmed/26263966 http://dx.doi.org/10.3390/molecules200813941 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Li, Zhibin
Chen, Shaohua
Zhu, Shaowen
Luo, Jianjun
Zhang, Yaomou
Weng, Qunfang
Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title_full Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title_fullStr Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title_full_unstemmed Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title_short Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives
title_sort synthesis and fungicidal activity of β-carboline alkaloids and their derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332272/
https://www.ncbi.nlm.nih.gov/pubmed/26263966
http://dx.doi.org/10.3390/molecules200813941
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