Abstract
A series of cinnamic acid esters and their derivatives were synthesized and evaluated for antifungal activities in vitro against four plant pathogenic fungi by using the mycelium growth rate method. Structure−activity relationship was derived also. Almost all of the compounds showed some inhibition activity on each of the fungi at 0.5 mM. Eight compounds showed the higher average activity with average EC50 values of 17.4–28.6 μg/mL for the fungi than kresoxim-methyl, a commercial fungicide standard, and ten compounds were much more active than commercial fungicide standards carbendazim against P. grisea or kresoxim-methyl against both P. grisea and Valsa mali. Compounds C1 and C2 showed the higher activity with average EC50 values of 17.4 and 18.5 μg/mL and great potential for development of new plant antifungal agents. The structure−activity relationship analysis showed that both the substitution pattern of the phenyl ring and the alkyl group in the alcohol moiety significantly influences the activity. There exists complexly comprehensive effect between the substituents on the phenyl ring and the alkyl group in the alcohol moiety on the activity. Thus, cinnamic acid esters showed great potential the development of new antifungal agents for plant protection due to high activity, natural compounds or natural compound framework, simple structure, easy preparation, low-cost and environmentally friendly.
Highlights
Plant mycosis is an important problem of agricultural production worldwide [1] and often results in severe yield losses and quality decrease of agricultural products
In order to know the effect of substitution patterns of the phenyl ring and the type of alkyl groups in the alcohol moiety on the activity, we firstly designed both A and B series of target compounds
A series consisting of 28 compounds is a class of ethyl cinnamate derivatives containing various substituents on the phenyl ring
Summary
Plant mycosis is an important problem of agricultural production worldwide [1] and often results in severe yield losses and quality decrease of agricultural products. Many of the fungi can harm animal and human health due to their mycotoxins [2]. Various fungicides have been extensively used to control fungal plant diseases in current agriculture. The prolonged usage of some antifungal agents can lead to drug resistance, environmental problems and residue toxicity [3]. It is necessary to develop environmentally friendly plant fungicides.
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
