Search: id:"swepub:oai:DiVA.org:umu-134612" >
N-Aryl-N'-ethylenea...
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Knutsson, SofieUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
(author)
N-Aryl-N'-ethyleneaminothioureas effectively inhibit acetylcholinesterase 1 from disease-transmitting mosquitoes
- Article/chapterEnglish2017
Publisher, publication year, extent ...
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Elsevier BV,2017
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Numbers
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LIBRIS-ID:oai:DiVA.org:umu-134612
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-134612URI
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https://doi.org/10.1016/j.ejmech.2017.03.050DOI
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https://urn.kb.se/resolve?urn=urn:nbn:se:ltu:diva-65167URI
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Language:English
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Summary in:English
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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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.
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Kindahl, TomasUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)toskil02
(author)
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Engdahl, CeciliaUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)ceen0001
(author)
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Nikjoo, Dariush,1977-Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:ltu)darnik
(author)
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Forsgren, NinaCBRN Defence and Security, Swedish Defence Research Agency
(author)
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Kitur, StanleyCentre for Biotechnology Research and Development, Kenya Medical Research Institute
(author)
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Ekström, FredrikCBRN Defence and Security, Swedish Defence Research Agency
(author)
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Kamau, LunaCentre for Biotechnology Research and Development, Kenya Medical Research Institute
(author)
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Linusson, AnnaUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)analin99
(author)
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Umeå universitetKemiska institutionen
(creator_code:org_t)
Related titles
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In:European Journal of Medicinal Chemistry: Elsevier BV134, s. 415-4270223-52341768-3254
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- By the author/editor
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Knutsson, Sofie
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Kindahl, Tomas
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Engdahl, Cecilia
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Nikjoo, Dariush, ...
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Forsgren, Nina
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Kitur, Stanley
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Ekström, Fredrik
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Kamau, Luna
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Linusson, Anna
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- NATURAL SCIENCES
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NATURAL SCIENCES
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European Journal ...
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Umeå University
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Luleå University of Technology