Barbara E. Kurys

Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase

Abstract A series of imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates was prepared and evaluated as dual acetylcholinesterase (AChE) and monoamine oxidase (MAO) inhibitors. Halogen substitution ortho to the carbamate functionality in the eight position resulted in a significant increase in binding affinity for both AChE and MAO-A.

Preparation of 3-(4-pyridinylamino)-1,2-benzisoxazoles via a nucleophilic aromatic substitution reaction

Abstract An efficient three step process for the preparation of secondary 3-amino-1,2-benzisoxazoles is described. The key step is the isomerization/cyclization of an ortho halo or nitro amidoxime. The nucleophilic substitution reaction is successful with a wide variety of substituents on the aromatic ring, including an electron donating substituent para to the site of attack.