Natural Products‐Based Fungicides: Synthesis and Antifungal Activity against Plant Pathogens of 2H‐Chromene Derivatives

Abstract

Aiming to search for novel potential antifungal agents, forty 2H‐chromene analogs were designed, synthesized and their antifungal activity against some typical plant pathogenic fungi were firstly evaluated. The in vitro antifungal bioassays showed that some of the target compounds exhibited comparable or better inhibition activities than the commercial agricultural fungicide hymexazol. Especially compound 1m displayed more promising fungicidal effect against Alternaria alternate (EC50=9.9 μg/mL) and Botrytis cinerea (EC50=9.4 μg/mL), which was significantly superior to hymexazol. Moreover, in vivo protective effects results also indicated that compound 1m had an excellent potential for further development as a new botanical pesticide.

Quinoline Alkaloids from the Roots of Orixa japonica with the Anti‐Pathogenic Fungi Activities

“…[4] In resent years, the discovery of botanical fungicides engaged the interests of scientists due to the advantages of high efficiency, low or no toxicity, easy degradation, high selectivity, and a low risk of inducing drug resistance to control plant diseases. [5,6] Orixa japonica (Rutaceae), widely distributed in China, Japan, and Korea, is used as pesticide in these countries, and its stems and leaves possessed potential insecticidal activities. [7 -11] Its chemical constituent was investigated previously, including quinoline alkaloids, coumarins, and terpenoids, which possessed good Supporting information for this article is available on the WWW under https://doi.org/10.1002/cbdv.202201097 Part of a Special Collection on Chemical Evidence/ Interpretation to Diverse Effects of Ethnomedicines of China.…”

“…However, those applications affected human health and polluted the environment [4] . In resent years, the discovery of botanical fungicides engaged the interests of scientists due to the advantages of high efficiency, low or no toxicity, easy degradation, high selectivity, and a low risk of inducing drug resistance to control plant diseases [5,6] …”

A Comprehensive Investigation of Hydrazide and Its Derived Structures in the Agricultural Fungicidal Field

“…In order to alleviate the problems mentioned above, while in line with the concept of green development, high quality, and sustainable development, researchers have done a lot of scientific research. For example, the development of nanopreparations in fungicides could effectively improve the utilization rate, increase the efficacy of the original drug, and reduce the impact on the environment. , In addition, the discovery and fungicidal application of microbial pesticides, natural products, RNA interference, and polypeptides could also meet the needs of green development. − Furthermore, the development of new green ecological fungicides could also delay the increase of pathogen resistance. , Meanwhile, structural modification based on natural products has become an effective way to develop new green agrochemicals, such as natural strobilurin A-derived methoxyacrylate fungicides, natural cinnamic acid-derived dimethomorph, and so on. − At present, although commercial fungicides have various structures, the fungicidal targets are same for the similar structures, which results in the existence of cross-resistance. Therefore, the discovery of new pharmacophores and the exploration of new targets are also very important for the development of fungicides …”

“…97−101 Furthermore, the development of new green ecological fungicides could also delay the increase of pathogen resistance. 102,103 Meanwhile, structural modification based on natural products has become an effective way to develop new green agrochemicals, such as natural strobilurin A-derived methoxyacrylate fungicides, natural cinnamic acidderived dimethomorph, and so on. 104−106 At present, although commercial fungicides have various structures, the fungicidal targets are same for the similar structures, which results in the existence of cross-resistance.…”

Synthesis and Antifungal Activity of Curcumol Derivatives

“…Therefore, there is an urgent need to develop more effective and environment‐friendly small molecule fungicides against plant pathogenic fungi. In recent decades, on account of the characteristics of high efficiency, low toxicity and environmental friendliness, direct application or structure modification of natural products has become an essential way to discover and create new fungicides [8–10] …”