Inhibitor profile of bis(n)-tacrines and N-methylcarbamates on acetylcholinesterase from Rhipicephalus (Boophilus) microplus and Phlebotomus papatasi.

Highlights: [•] Carbamates were selective for tick & sand fly acetylcholinesterase over that of human & bovine. [•] Tick had 1000-fold lower sensitivity toward tacrine than all previous species tested. [•] In tick, the W384 residue has a structural clash with tacrine and related inhibitors. [•] There is little resistance to coumaphos oxon and carbamates in AChE from field strains. [•] One compound, 2-((2-ethylbutyl)thio)phenyl methylcarbamate, is an excellent new lead. [Copyright &y& Elsevier]