Studies on Cognitive Enhancing Agents. III. Antiamnestic and Antihypoxic Activities of a Series of l-Bicycloaryl-2-(.OMEGA.-aminoalkoxy)ethanols

Autor:	Hisaaki Chaki, Yozo Todo, Hirokazu Narita, Tetsuo Yamafuji, Kazunori Kitamura, Masaru Tai, Hajime Morita, Mutsuko Maekawa, Naomi Okada, Satoshi Ono
Rok vydání:	1995
Předmět:	Indole test Ethanol Bicyclic molecule Stereochemistry General Chemistry General Medicine Chemical synthesis Acute toxicity chemistry.chemical_compound chemistry Tacrine Drug Discovery medicine Potency Benzofuran medicine.drug
Zdroj:	Chemical and Pharmaceutical Bulletin. 43:1492-1496
ISSN:	1347-5223 0009-2363
DOI:	10.1248/cpb.43.1492
Popis:	2-(2-Aminoethoxy)-1-hydroxyethyl derivatives of bicyclic arenes (naphthalene, thianaphthene, benzofuran, and indole) were prepared and screened for antiamnestic (AA) and antihypoxic (AH) activities which were evaluated by measuring the reversing potency in electroconvulsion-induced amnesia and the protective effect against hypoxia, respectively, in mice. Compound 3o, 1-(benzo[b]thiophen-5-yl)-2- (2-diethylaminoethoxy)ethanol, showed the best AA and AH activity profile, being superior to our prototype compound, 2-(2-dimethylaminoethoxy)-1-phenylethanol (1). Elongation of the ethylene linkage in the side chain of 3o to 3- and 4-carbon moieties brought about a significant decrease in AH activity. Compound 3o was further investigated for its protective effect against CO2-induced memory impairment and for acute toxicity in mice. It is ten-fold more potent than tacrine in the amnesia-reversal assay and is considerably less toxic than tacrine.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::558d6321c59f09e5eb926266aec24582 https://doi.org/10.1248/cpb.43.1492 Zobrazit plný text záznamu