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3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.

Abstract：

:A series of 26 derivatives of the novel muscarinic antagonist 3-(2-benzofuranyl)quinuclidin-2-ene (1) has been synthesized and evaluated for muscarinic and antimuscarinic properties. The affinity of the compounds was determined by competition experiments in homogenates of cerebral cortex, heart, parotid gland, and urinary bladder from guinea pigs using (-)-[3H]-3-quinuclidinyl benzilate as the radioligand, and the antimuscarinic-potency was determined in a functional assay on isolated guinea pig urinary bladder using carbachol as the agonist. The 5-fluorobenzofuranyl derivative was slightly more potent than 1. The 7-bromo-substituted 8 displayed a 14-fold tissue selectivity ratio for muscarinic receptors in the cortex versus the parotid gland. Comparative molecular field analysis and quantitative structure-activity relationship models were developed for this series of substituted benzofuranyl derivatives.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Nordvall G,Sundquist S,Johansson G,Glas G,Nilvebrant L,Hacksell U

doi

10.1021/jm950455c

subject

Has Abstract

pub_date

1996-08-16 00:00:00

pages

3269-77

issue

17

eissn

0022-2623

issn

1520-4804

pii

jm950455c

journal_volume

39

pub_type

杂志文章

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