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Synthesis and structure—activity relationships of new muscarinic antagonists

✍ Scribed by Victor I. Cohen; Raymond E. Gibson; Richard C. Reba

Publisher
John Wiley and Sons
Year
1987
Tongue
English
Weight
313 KB
Volume
76
Category
Article
ISSN
0022-3549

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✦ Synopsis

In an attempt to develop more selective muscarinic acetylcholine receptor (m-AcChR) antagonists, (R)-1-azabicyclo[2.2.2]oct-3-yl-thioxanthene-9-carboxylate, (R,S)-thiochromane-4-carboxylate, and (R,S)-chromane-4-carboxylate were synthesized. Evaluation of the binding affinities of these compounds to muscarinic receptors indicates that replacing the oxygen by sulfur in the xanthenyl and chromanyl moieties does not significantly change selectivity, but does reduce the affinity of 5 and enhance the affinity of 9a.

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