5, 7-Dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl] ethyl]-6H-pyrrolo [3, 2-f]-1, 2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase
A Villalobos, TW Butler, DS Chapin…
文献索引：Villalobos; Butler; Chapin; Chen; DeMattos; Ives; Jones; Liston; Nagel; Nason; Nielsen; Ramirez; Shalaby; White Journal of Medicinal Chemistry, 1995 , vol. 38, # 15 p. 2802 - 2808
A series of N-benzylpiperidines (2a-d, 10) with novel isoxazole-containing tricycles has been prepared. This series has shown potent in vitro inhibition of the enzyme acetylcholinesterase (AChE), with Ic5oS= 0.33-3.6 nM. Compound 2a was the most potent inhibitor with an IC50= 0.33 f 0.09 nM. Derivatives 2a-d and 10 displayed weak in vitro inhibition of butyrylcholinesterase (BuChE) with ICBOs= 600-23 000 nM. The most ...
