Reduction of malaria transmission in sub-Saharan Africa depends heavily on the use of insecticide-treated nets. At present only pyrethroid insecticides are used on these nets, but the emergence of pyrethroid-resistant mosquitoes has seriously jeopardized this disease control method.  To identify a potential new class of insecticides that are safe for use on nets, we have been exploring the titled structures, to identify compounds that are highly selective for inhibition of An. gambiae acetylcholinesterase over the human enzyme. An additional design goal is to potently inhibit the G119S resistant mutant of the mosquito enzyme. Modulation of the heterocycle and substituents can confer both high enzymatic selectivity, and good toxicity to the wild-type and G119S mutant malaria mosquito

Small ring heterocyclic carbamates and carboxamides: The search for species-selective acetylcholinesterase inhibitors against the malaria mosquito

243rd National Meeting (2012)

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