Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogs

…, J Nielsen, K Hedberg, A Dunaiskis…

Index: Chen; Nielsen; Hedberg; Dunaiskis; Jones; Russo; Johnson; Ives; Liston Journal of Medicinal Chemistry, 1992 , vol. 35, # 8 p. 1429 - 1434

Full Text: HTML

Citation Number: 38

Abstract

The synthesis of a series of 1, 2, 3, 3a, 8, 8a-hexahydroindeno [2, 1-b] pyrrole 5- alkylcarbamates and their reaolution are reported. These compounds are structurally related to physostigmine with substitution of a methylene group in place of the NMe group at position 8 of physostigmine. Many of these 8-carbaphysostigmine analogues are more potent acetylcholinesterase inhibitors in vitro and less toxic in vivo than physostigmine. ...