Format

Send to

Choose Destination
J Med Chem. 2008 Oct 9;51(19):5915-8. doi: 10.1021/jm800935u. Epub 2008 Sep 18.

Discovery of biphenyl piperazines as 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

A series of novel biphenyl piperazines was discovered as highly potent muscarinic acetylcholine receptor antagonists via high throughput screening and subsequent optimization. Compound 5c with respective 500- and 20-fold subtype selectivity for M3 over M2 and M1 exhibited excellent inhibitory activity and long duration of action in a bronchoconstriction in vivo model in mice via intranasal administration. The novel inhaled mAChR antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease.

PMID:
18798607
DOI:
10.1021/jm800935u
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for American Chemical Society
Loading ...
Support Center