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SAR Studies on the Potent and Selective Muscarinic Antagonist 2-Ethylthio-2,2-diphenylacetic Acid N,N-Diethylaminoethyl Ester

✍ Scribed by Serena Scapecchi; Piero Angeli; Silvia Dei; Carla Ghelardini; Fulvio Gualtieri; Gabriella Marucci; Fiorella Paparelli; M. Novella Romanelli; Elisabetta Teodori

Book ID: 102750465
Publisher: John Wiley and Sons
Year: 1997
Tongue: English
Weight: 542 KB
Volume: 330
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19973300503

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✦ Synopsis

Molecular modification of the potent and selective muscarinic antagonist 2-ethylthio-2,2-diphenylacetic acid N,N-diethylaminoethyl ester was performed in order to identify M2 selective antagonists able to cross the blood brain barrier and potentially useful in the treatment of Alzheimer's disease. Modifications included substitution or hydrogenation of one of the phenyl rings as well as their incorporation in a tricyclic system. In general the changes introduced were detrimental for both affinity and selectivity. Only a modest M2 selectivity is present in some compounds that, on the other hand, carry a quaternary ammonium group which precludes their penetration into the brain.

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