9-Amino-1, 2, 3, 4-tetrahydroacridin-1-ols. Synthesis and evaluation as potential Alzheimer's disease therapeutics

…, KJ Kapples, ML Cornfeldt, MR Szewczak…

Index: Shutske; Pierrat; Kapples; Cornfeldt; Szewczak; Huger; Bores; Haroutunian; Davis Journal of Medicinal Chemistry, 1989 , vol. 32, # 8 p. 1805 - 1813

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Citation Number: 92

Abstract

The synthesis of a series of 9-amino-1, 2, 3, 4-tetrahydroacridin-l-ols is reported. These compounds are related to 1, 2, 3, 4-tetrahydro-9-acridinamine (THA, tacrine). They inhibit acetylcholinesterase in vitro and are active in a model that may be predictive of activity in Alzheimer's disease-the scopolamine-induced impairment of 24-h memory of a passive dark- avoidance paradigm in mice. Two compounds,(i)-9-amino-1, 2, 3, 4-tetrahydroacridin-l-01 ...