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N-Aryl-N'-ethyleneaminothioureas effectively inhibit acetylcholinesterase 1 from disease-transmitting mosquitoes
Department of Chemistry, Umeå University.
Department of Chemistry, Umeå University.
Department of Chemistry, Umeå University.
Department of Chemistry, Umeå University.ORCID iD: 0000-0002-4628-3857
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2017 (English)In: European Journal of Medicinal Chemistry, ISSN 0223-5234, E-ISSN 1768-3254, Vol. 134, p. 415-427Article in journal (Refereed) Published
Abstract [en]

Vector control of disease-transmitting mosquitoes by insecticides has a central role in reducing the number of parasitic- and viral infection cases. The currently used insecticides are efficient, but safety concerns and the development of insecticide-resistant mosquito strains warrant the search for alternative compound classes for vector control. Here, we have designed and synthesized thiourea-based compounds as non-covalent inhibitors of acetylcholinesterase 1 (AChE1) from the mosquitoes Anopheles gambiae (An. gambiae) and Aedes aegypti (Ae. aegypti), as well as a naturally occurring resistant-conferring mutant. The N-aryl-N’-ethyleneaminothioureas proved to be inhibitors of AChE1; the most efficient one showed submicromolar potency. Importantly, the inhibitors exhibited selectivity over the human AChE (hAChE), which is desirable for new insecticides. The structure-activity relationship (SAR) analysis of the thioureas revealed that small changes in the chemical structure had a large effect on inhibition capacity. The thioureas showed to have different SAR when inhibiting AChE1 and hAChE, respectively, enabling an investigation of structure-selectivity relationships. Furthermore, insecticidal activity was demonstrated using adult and larvae An. gambiae and Ae. aegypti mosquitoes.

Place, publisher, year, edition, pages
Elsevier, 2017. Vol. 134, p. 415-427
National Category
Medical and Health Sciences Other Materials Engineering
Research subject
Engineering Materials
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URN: urn:nbn:se:ltu:diva-65167DOI: 10.1016/j.ejmech.2017.03.050ISI: 000401677500035PubMedID: 28433681Scopus ID: 2-s2.0-85017625955OAI: oai:DiVA.org:ltu-65167DiVA, id: diva2:1134011
Available from: 2017-08-17 Created: 2017-08-17 Last updated: 2018-03-05Bibliographically approved

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