Abstract
Umbelliferone was discovered to be an important allelochemical in our previous study, but the contribution of its activity and structure has not yet been revealed. In this study, a series of analogues were synthesized to determine the skeleton of umbelliferone and examine its fungicidal activity. Furthermore, targeted modifications were conducted with three plant parasitic fungi to examine the lead compounds. Among those tested, compounds 2f and 10 were found to show excellent antifungal activity with an inhibitory rate over 80% at 100 ug/mL. The study proves that umbelliferone can be a promising skeleton for fungicides discovery. In addition, the primary structure–activity relationship provides a good guidance for the discovery of novel fungicides based on natural products in the future.
Highlights
Plant pathogenic fungi have jeopardized crop yields and food security globally
The crude products were prepared by filtering the mixture and evaporating the solvent and were further purified by silica chromatography (CHCl3 /MeOH 50/1) to give compounds 2c–g (Scheme 1)
The crude products were further purified by silica chromatography (CHCl3 /MeOH 50/1) to give compounds 3a–d and 4a–d (Scheme 2)
Summary
Fungicides have always been an efficient way of minimizing the cost of plant diseases [1]. The widespread use of traditional fungicides has led to increased resistance, mammalian toxicity, and a threat to the environment. This has stimulated the demand for integrated control measures with more selective, lower dose agents that have improved resistance [2,3,4,5]. Natural products (NPs) have been a rich source of novel fungicide development either with direct application or serving as a model for advanced modification [6]. There is an urgent need for cost-effective tactics, instead of “blind search”, in the development of new fungicides [7]
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