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Bioorg Med Chem Lett. 2012 May 1;22(9):3366-9. doi: 10.1016/j.bmcl.2012.02.015. Epub 2012 Feb 15.

Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.

Author information

1
GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA.

Abstract

A novel series of N-substituted tropane derivatives was characterized as potent muscarinic acetylcholine receptor antagonists (mAChRs). Kinetic washout studies showed that the N-endosubstituted analog 24 displayed much slower reversibility at mAChRs than the methyl-substituted parent molecule darotropium. In addition, it was shown that this characteristic appeared to translate into enhanced which duration of action in a mouse model of bronchonstriction.

PMID:
22460029
DOI:
10.1016/j.bmcl.2012.02.015
[Indexed for MEDLINE]

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