Total synthesis and structure-activity-relationship of Alternaric acid delivers an herbicide vector
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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.
Israel , E M , Comas-Barceló , J , Slawin , A M Z & Watson , A J B 2022 , ' Total synthesis and structure-activity-relationship of Alternaric acid delivers an herbicide vector ' , Nature Synthesis , vol. First Online . https://doi.org/10.1038/s44160-022-00169-3
Copyright © 2022, The Author(s), under exclusive licence to Springer Nature Limited . For the purpose of open access, the author has applied a Creative Commons Attribution (CC BY) public copyright Licence to any Accepted Author Manuscript version arising. The final published version of this work is available at https://doi.org/10.1038/s44160-022-00169-3
DescriptionE.M.I and A.J.B.W. thank Syngenta and EPSRC for an iCASE PhD studentship.
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