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Angew Chem Int Ed Engl. 2017 Aug 7;56(33):9881-9885. doi: 10.1002/anie.201705400. Epub 2017 Jul 12.

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

Author information

1
School of Molecular Sciences, University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
2
ARC Centre of Excellence in Plant Energy Biology, University of Western Australia, 35 Stirling Highway, Crawley, WA, 6009, Australia.
3
BASF SE, 67056, Ludwigshafen am Rhein, Germany.

Abstract

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.

KEYWORDS:

Arabidopsis; drug discovery; herbicides; malaria

PMID:
28654179
DOI:
10.1002/anie.201705400

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