Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides

Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a co...

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Bibliographic Details
Published in:Angewandte Chemie 2017-08, Vol.129 (33), p.10013-10017
Main Authors: Corral, Maxime G., Leroux, Julie, Tresch, Stefan, Newton, Trevor, Stubbs, Keith A., Mylne, Joshua S.
Format: Article
Language:English
Subjects:
Antimalarial agents
Arabidopsis
Chemistry
Drug development
Drugs
Herbicide resistance
Herbicides
Herbizide
Lead compounds
Libraries
Malaria
Medicinal plants
Parasites
Photosystem II
Scaffolds
Vector-borne diseases
Viability
Weeds
Wirkstoffentwicklung
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Summary:Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post‐emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides. Zweckentfremdet: Die evolutionäre Beziehung zwischen Apicomplexa‐Parasiten und Pflanzen, Antimalariawirkstoffe, die Modellpflanze Arabidopsis thaliana und eine Sammlung physikochemischer Daten bekannter Herbizide führten in Kombination zu einer Verbindung, die ähnlich stark gegen aufgegangene Unkräuter wirkt wie kommerzielle Herbizide. Dadurch wird bestätigt, dass Antimalariaverbindungen taugliche Leitstrukturen für die Herbizid‐Entwicklung sind.
ISSN:0044-8249
1521-3757
DOI:10.1002/ange.201705400