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N-Aryl-N'-ethylenea...
N-Aryl-N'-ethyleneaminothioureas effectively inhibit acetylcholinesterase 1 from disease-transmitting mosquitoes
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- Knutsson, Sofie (author)
- Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
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- Kindahl, Tomas (author)
- Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
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- Engdahl, Cecilia (author)
- Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
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- Nikjoo, Dariush, 1977- (author)
- Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
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- Forsgren, Nina (author)
- CBRN Defence and Security, Swedish Defence Research Agency
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- Kitur, Stanley (author)
- Centre for Biotechnology Research and Development, Kenya Medical Research Institute
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- Ekström, Fredrik (author)
- CBRN Defence and Security, Swedish Defence Research Agency
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- Kamau, Luna (author)
- Centre for Biotechnology Research and Development, Kenya Medical Research Institute
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- Linusson, Anna (author)
- Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University
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(creator_code:org_t)
- Elsevier BV, 2017
- 2017
- English.
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In: European Journal of Medicinal Chemistry. - : Elsevier BV. - 0223-5234 .- 1768-3254. ; 134, s. 415-427
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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https://urn.kb.se/re...
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Abstract
Subject headings
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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.
Subject headings
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
Keyword
- Acetylcholinesterase 1
- Aedes aegypti
- Anopheles gambiae
- Insecticides
- Thiourea
- Vector control
Publication and Content Type
- ref (subject category)
- art (subject category)
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To the university's database
- 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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show more...
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Ekström, Fredrik
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Kamau, Luna
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Linusson, Anna
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show less...
- About the subject
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- NATURAL SCIENCES
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NATURAL SCIENCES
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and Chemical Science ...
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and Organic Chemistr ...
- Articles in the publication
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European Journal ...
- By the university
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Umeå University
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Luleå University of Technology