Tricyclic cyanoguanidines: synthesis, site of action and insecticidal activity of a novel class of reversible acetylcholinesterase inhibitors
BL Finkelstein, EA Benner, MC Hendrixson…
文献索引：Finkelstein, Bruce L.; Benner, Eric A.; Hendrixson, Maura C.; Kranis, Kevin T.; Rauh, James J.; Sethuraman, Maya R.; McCann, Stephen F. Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 3 p. 599 - 613
Bridged-tricyclic cyanoguanidines 1 were found to be active as insecticides. The preparation and structure–activity relationships of oxacyclic (X= O) and carbocyclic (X= CH2) analogues of 1 is described. Compounds 1 were found to inhibit acetylcholinesterase with IC50 values comparable to the organophosphate Paraoxon. Unlike organophosphates, cyanoguanidines 1 were shown to reversibly bind acetylcholinesterase. This mode of ...
