Format

Send to

Choose Destination
J Med Chem. 2008 Aug 28;51(16):4866-9. doi: 10.1021/jm800634k. Epub 2008 Aug 5.

Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.

Author information

1
GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA. jianjin@unc.edu

Abstract

High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.

PMID:
18680280
DOI:
10.1021/jm800634k
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center