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Structure-activity ...
Structure-activity relationships reveal beneficial selectivity profiles of inhibitors targeting acetylcholinesterase of disease-transmitting mosquitoes
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- Vidal-Albalat, Andreu (författare)
- Umeå universitet,Kemiska institutionen
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- Kindahl, Tomas, 1980- (författare)
- Umeå universitet,Kemiska institutionen
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- Rajeshwari, Rajeshwari (författare)
- Umeå universitet,Kemiska institutionen
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- Lindgren, Cecilia (författare)
- Umeå universitet,Kemiska institutionen
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- Forsgren, Nina (författare)
- CBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden
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- Kitur, Stanley (författare)
- Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
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- Tengo, Laura Sela (författare)
- Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
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- Ekström, Fredrik (författare)
- CBRN Defence and Security, Swedish Defence Research Agency, Umeå, Sweden
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- Kamau, Luna (författare)
- Centre for Biotechnology Research and Development, Kenya Medical Research Institute, Nairobi, Kenya
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- Linusson, Anna, 1970- (författare)
- Umeå universitet,Kemiska institutionen
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(creator_code:org_t)
- American Chemical Society (ACS), 2023
- 2023
- Engelska.
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Ingår i: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 66:9, s. 6333-6353
- Relaterad länk:
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https://doi.org/10.1...
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https://umu.diva-por... (primary) (Raw object)
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- 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.
Ämnesord
- NATURVETENSKAP -- Kemi -- Organisk kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences -- Organic Chemistry (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
Publikations- och innehållstyp
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- art (ämneskategori)
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Till lärosätets databas
- Av författaren/redakt...
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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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visa fler...
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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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visa färre...
- Om ämnet
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- NATURVETENSKAP
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NATURVETENSKAP
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och Kemi
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och Organisk kemi
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Medicinska och f ...
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och Läkemedelskemi
- Artiklar i publikationen
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Journal of Medic ...
- Av lärosätet
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Umeå universitet