ArticlePloS one2012
Select small core structure carbamates exhibit high contact toxicity to "carbamate-resistant" strain malaria mosquitoes, Anopheles gambiae (Akron).
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 36 citations in OpenAlex.
- Potent and selective indole-based inhibitors targeting disease-transmitting mosquitoes.RSC medicinal chemistry · 2026Article
- Defining the genetics of the widely used G3 strain of the mosquito, Anopheles gambiae.Scientific reports · 2025Article
- Mosquito mutations F290V and F331W expressed in acetylcholinesterase of the sand fly Phlebotomus papatasi (Scopoli): biochemical properties and inhibitor sensitivity.Parasites & vectors · 2025Article
- Structure-Activity Relationships Reveal Beneficial Selectivity Profiles of Inhibitors Targeting Acetylcholinesterase of Disease-Transmitting Mosquitoes.Journal of medicinal chemistry · 2023Article
- CuI-Catalyzed Coupling Reactions of 4-Iodopyrazoles and Alcohols: Application toward Withasomnine and Homologs.Molecules (Basel, Switzerland) · 2021Article
- Cysteine-Targeted Insecticides againstACS medicinal chemistry letters · 2020Article
- Mosquito Acetylcholinesterase as a Target for Novel Phenyl-Substituted Carbamates.International journal of environmental research and public health · 2019Article
- Select β- and γ-branched 1-alkylpyrazol-4-yl methylcarbamates exhibit high selectivity for inhibition ofPesticide biochemistry and physiology · 2018Article
- Structure of the G119S Mutant Acetylcholinesterase of the Malaria Vector Anopheles gambiae Reveals Basis of Insecticide Resistance.Structure (London, England : 1993) · 2018Article
- Discovery of Species-selective and Resistance-breaking Anticholinesterase Insecticides for the Malaria Mosquito.Current medicinal chemistry · 2017Review
- An insecticide resistance-breaking mosquitocide targeting inward rectifier potassium channels in vectors of Zika virus and malaria.Scientific reports · 2016Article
- Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase.Bioorganic & medicinal chemistry letters · 2015Article
- Carbamate and pyrethroid resistance in the akron strain of Anopheles gambiae.Pesticide biochemistry and physiology · 2015Article
- 3-Oxoisoxazole-2(3H)-carboxamides and isoxazol-3-yl carbamates: Resistance-breaking acetylcholinesterase inhibitors targeting the malaria mosquito, Anopheles gambiae.Bioorganic & medicinal chemistry · 2015Article
- Article
- Design, Synthesis, and Evaluation of Genistein Analogues as Anti-Cancer Agents.Anti-cancer agents in medicinal chemistry · 2015Article
- Acetylcholinesterase of the sand fly, Phlebotomus papatasi (Scopoli): construction, expression and biochemical properties of the G119S orthologous mutant.Parasites & vectors · 2014Article
- CYP6 P450 enzymes and ACE-1 duplication produce extreme and multiple insecticide resistance in the malaria mosquito Anopheles gambiae.PLoS genetics · 2014Article
- Article
- Aryl methylcarbamates: potency and selectivity towards wild-type and carbamate-insensitive (G119S) Anopheles gambiae acetylcholinesterase, and toxicity to G3 strain An. gambiae.Chemico-biological interactions · 2013Article
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Authors and funding
16 authors at 3 institutions in 1 country.
Funding
Abstract
Acetylcholinesterase (AChE) is a proven target for control of the malaria mosquito (Anopheles gambiae). Unfortunately, a single amino acid mutation (G119S) in An. gambiae AChE-1 (AgAChE) confers resistance to the AChE inhibitors currently approved by the World Health Organization for indoor residual spraying. In this report, we describe several carbamate inhibitors that potently inhibit G119S AgAChE and that are contact-toxic to carbamate-resistant An. gambiae. PCR-RFLP analysis was used to confirm that carbamate-susceptible G3 and carbamate-resistant Akron strains of An. gambiae carry wild-type (WT) and G119S AChE, respectively. G119S AgAChE was expressed and purified for the first time, and was shown to have only 3% of the turnover number (k(cat)) of the WT enzyme. Twelve carbamates were then assayed for inhibition of these enzymes. High resistance ratios (>2,500-fold) were observed for carbamates bearing a benzene ring core, consistent with the carbamate-resistant phenotype of the G119S enzyme. Interestingly, resistance ratios for two oxime methylcarbamates, and for five pyrazol-4-yl methylcarbamates were found to be much lower (4- to 65-fold). The toxicities of these carbamates to live G3 and Akron strain An. gambiae were determined. As expected from the enzyme resistance ratios, carbamates bearing a benzene ring core showed low toxicity to Akron strain An. gambiae (LC(50)>5,000 μg/mL). However, one oxime methylcarbamate (aldicarb) and five pyrazol-4-yl methylcarbamates (4a-e) showed good to excellent toxicity to the Akron strain (LC(50) = 32-650 μg/mL). These results suggest that appropriately functionalized "small-core" carbamates could function as a resistance-breaking anticholinesterase insecticides against the malaria mosquito.
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