Nematicidal and insecticidal activities of halogenated indoles View Full Text


Ontology type: schema:ScholarlyArticle      Open Access: True


Article Info

DATE

2019-12

AUTHORS

Satish Kumar Rajasekharan, Jin-Hyung Lee, Vinothkannan Ravichandran, Jin-Cheol Kim, Jae Gyu Park, Jintae Lee

ABSTRACT

Parasite death via ion channel activations is the hallmark of anthelmintic and antiparasitic drugs. Glutamate gated chloride channel (GluCl) is a prominent targets for drug selection and design in parasitology. We report several iodine-fluorine based lead activators of GluCl by computational studies and structure-activity relationship analysis. 5-Fluoro-4-iodo-1H-pyrrolo [2, 3-b] pyridine and 5-iodoindole were bioactive hits that displayed in vitro anthelmintic and insecticidal activities against Bursaphelenchus xylophilus, Meloidogyne incognita, and Tenebrio molitor. Two important findings stood out: (i) 5F4IPP induced parasite death, and interacted proficiently with Gln219 amino acid of pentameric GluCl in docking analysis, and (ii) 5-iodoindole appeared to act by forming giant vacuoles in nematodes, which led to a form of non-apoptotic death known as methuosis. The study suggests halogenated-indoles and 1H-pyrrolo [2, 3-b] pyridine derivatives be regarded potential biocides for plant-parasitic nematodes and insects, and warrants further research on the mode of actions, and field investigations. More... »

PAGES

2010

Identifiers

URI

http://scigraph.springernature.com/pub.10.1038/s41598-019-38561-3

DOI

http://dx.doi.org/10.1038/s41598-019-38561-3

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1112135350

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/30765810


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