SwePub
Sök i LIBRIS databas

  Extended search

onr:"swepub:oai:DiVA.org:umu-208264"
 

Search: onr:"swepub:oai:DiVA.org:umu-208264" > Structure-activity ...

  • 1 of 1
  • Previous record
  • Next record
  •    To hitlist
  • Vidal-Albalat, AndreuUmeå universitet,Kemiska institutionen (author)

Structure-activity relationships reveal beneficial selectivity profiles of inhibitors targeting acetylcholinesterase of disease-transmitting mosquitoes

  • Article/chapterEnglish2023

Publisher, publication year, extent ...

  • American Chemical Society (ACS),2023
  • electronicrdacarrier

Numbers

  • LIBRIS-ID:oai:DiVA.org:umu-208264
  • https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-208264URI
  • https://doi.org/10.1021/acs.jmedchem.3c00234DOI

Supplementary language notes

  • Language:English
  • Summary in:English

Part of subdatabase

Classification

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

Notes

  • Insecticide resistance jeopardizes the prevention of infectious diseases such as malaria and dengue fever by vector control of disease-transmitting mosquitoes. Effective new insecticidal compounds with minimal adverse effects on humans and the environment are therefore urgently needed. Here, we explore noncovalent inhibitors of the well-validated insecticidal target acetylcholinesterase (AChE) based on a 4-thiazolidinone scaffold. The 4-thiazolidinones inhibit AChE1 from the mosquitoes Anopheles gambiae and Aedes aegypti at low micromolar concentrations. Their selectivity depends primarily on the substitution pattern of the phenyl ring; halogen substituents have complex effects. The compounds also feature a pendant aliphatic amine that was important for activity; little variation of this group is tolerated. Molecular docking studies suggested that the tight selectivity profiles of these compounds are due to competition between two binding sites. Three 4-thiazolidinones tested for in vivo insecticidal activity had similar effects on disease-transmitting mosquitoes despite a 10-fold difference in their in vitro activity.

Subject headings and genre

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

  • Kindahl, Tomas,1980-Umeå universitet,Kemiska institutionen(Swepub:umu)toskil02 (author)
  • Rajeshwari, RajeshwariUmeå universitet,Kemiska institutionen(Swepub:umu)rara0074 (author)
  • Lindgren, CeciliaUmeå universitet,Kemiska institutionen(Swepub:umu)celi0013 (author)
  • Forsgren, NinaCBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden (author)
  • Kitur, StanleyCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya (author)
  • Tengo, Laura SelaCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya (author)
  • Ekström, FredrikCBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden (author)
  • Kamau, LunaCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya (author)
  • Linusson, Anna,1970-Umeå universitet,Kemiska institutionen(Swepub:umu)analin99 (author)
  • Umeå universitetKemiska institutionen (creator_code:org_t)

Related titles

  • In:Journal of Medicinal Chemistry: American Chemical Society (ACS)66:9, s. 6333-63530022-26231520-4804

Internet link

Find in a library

To the university's database

  • 1 of 1
  • Previous record
  • Next record
  •    To hitlist

Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.

 
pil uppåt Close

Copy and save the link in order to return to this view