Total synthesis and structure-activity-relationship of Alternaric acid delivers an herbicide vector

Eva M. Israel, Júlia Comas-Barceló, Alexandra M. Z. Slawin, Allan J. B. Watson

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Abstract

Global food security is one of the foremost challenges of our time and requires a multifaceted solution. Crop protection strategies are an essential part of this response; however, there is increasing resistance to known modes of action. Since its discovery in 1949, the natural product alternaric acid has been proposed as a starting point for herbicide development. However, this target is undeveloped due to its poor synthetic accessibility and a lack of knowledge of the associated pharmacology. Here we report the discovery of herbicidal compounds from alternaric acid that operate via a potentially unknown mode of action. Development of a total synthesis enabled structure–activity relationship profiling of compound libraries, which, combined with phenotypic screening and molecular modelling data, identified small-molecule lead compounds with enhanced and broader spectrum herbicidal activity than alternaric acid.
Original languageEnglish
JournalNature Synthesis
VolumeFirst Online
Early online date13 Oct 2022
DOIs
Publication statusE-pub ahead of print - 13 Oct 2022

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