✦ LIBER ✦

Synthesis and nicotinic acetylcholine receptor affinity of bivalent tropane-3-carboxylates

✍ Scribed by Suhong Zhang; Jie Cheng; Ying Liu; Liang Xu; Mark L. Trudell; Sari Izenwasser; Dean Wade

Publisher: Journal of Heterocyclic Chemistry
Year: 2007
Tongue: English
Weight: 363 KB
Volume: 44
Category: Article
ISSN: 0022-152X
DOI: 10.1002/jhet.5570440629

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✦ Synopsis

Abstract

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A series of diol di‐(tropane‐3α‐carboxylate) esters and diol di‐(tropane‐3β‐carboxylate) esters were synthesized from 3‐tropene‐3‐carboxylic acid and tropane‐3β‐carboxylic acid, respectively. The bivalent tropane‐3‐carboxylates were evaluated for their ability to inhibit [^3^H]cytisine binding at rat brain nicotinic acetylcholine receptors (nAChRs). In general the (3β,3β')‐isomers were more potent than (3α,3α')‐isomer and the (3β,3β')‐decyl derivative (n = 10, K~i~ = 145 nM) exhibited the most potent affinity for nAChRs of the series.

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