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Structure-activity ...
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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 ...
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American Chemical Society (ACS),2023
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electronicrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:umu-208264
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-208264URI
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https://doi.org/10.1021/acs.jmedchem.3c00234DOI
Supplementary language notes
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Language:English
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Summary in:English
Part of subdatabase
Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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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 ...)
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Kindahl, Tomas,1980-Umeå universitet,Kemiska institutionen(Swepub:umu)toskil02
(author)
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Rajeshwari, RajeshwariUmeå universitet,Kemiska institutionen(Swepub:umu)rara0074
(author)
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Lindgren, CeciliaUmeå universitet,Kemiska institutionen(Swepub:umu)celi0013
(author)
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Forsgren, NinaCBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden
(author)
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Kitur, StanleyCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
(author)
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Tengo, Laura SelaCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
(author)
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Ekström, FredrikCBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden
(author)
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Kamau, LunaCentre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
(author)
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Linusson, Anna,1970-Umeå universitet,Kemiska institutionen(Swepub:umu)analin99
(author)
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Umeå universitetKemiska institutionen
(creator_code:org_t)
Related titles
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In:Journal of Medicinal Chemistry: American Chemical Society (ACS)66:9, s. 6333-63530022-26231520-4804
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Vidal-Albalat, A ...
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Kindahl, Tomas, ...
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Rajeshwari, Raje ...
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Lindgren, Cecili ...
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Forsgren, Nina
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Kitur, Stanley
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Tengo, Laura Sel ...
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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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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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Umeå University