Article
Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase.
Bioorganic & medicinal chemistry letters - 15 Oct 2015
Camerino Eugene, Wong Dawn M, Tong Fan, Körber Florian, Gross Aaron D, Islam Rafique, Viayna Elisabet, Mutunga James M, Li Jianyong, Totrov Maxim M, Bloomquist Jeffrey R, Carlier Paul R
Abstract excerpt
Malaria is a devastating disease in sub-Saharan Africa, and current vector control measures are threatened by emerging resistance mechanisms. With the goal of developing new, selective, resistance-breaking insecticides we explored α-fluorinated methyl ketones as reversible covalent inhibitors of Anopheles gambiae acetylcholinesterase (AgAChE). Trifluoromethyl ketones 5 demonstrated remarkable volatility in...
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