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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 ...

  • Elsevier BV,2017
  • printrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:umu-134612
  • https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-134612URI
  • https://doi.org/10.1016/j.ejmech.2017.03.050DOI
  • https://urn.kb.se/resolve?urn=urn:nbn:se:ltu:diva-65167URI

Supplementary language notes

  • Language:English
  • Summary in:English

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  • Subject category:ref swepub-contenttype
  • Subject category:art swepub-publicationtype

Notes

  • 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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Added entries (persons, corporate bodies, meetings, titles ...)

  • Kindahl, TomasUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)toskil02 (author)
  • Engdahl, CeciliaUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)ceen0001 (author)
  • Nikjoo, Dariush,1977-Umeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:ltu)darnik (author)
  • Forsgren, NinaCBRN Defence and Security, Swedish Defence Research Agency (author)
  • Kitur, StanleyCentre for Biotechnology Research and Development, Kenya Medical Research Institute (author)
  • Ekström, FredrikCBRN Defence and Security, Swedish Defence Research Agency (author)
  • Kamau, LunaCentre for Biotechnology Research and Development, Kenya Medical Research Institute (author)
  • Linusson, AnnaUmeå universitet,Kemiska institutionen,Department of Chemistry, Umeå University(Swepub:umu)analin99 (author)
  • Umeå universitetKemiska institutionen (creator_code:org_t)

Related titles

  • In:European Journal of Medicinal Chemistry: Elsevier BV134, s. 415-4270223-52341768-3254

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