The discovery of AZD9164, a novel muscarinic M3 antagonist

Antonio Mete; Keith Bowers; Eric Chevalier; David K Donald; Helen Edwards; Katherine J Escott; Rhonan Ford; Ken Grime; Ian Millichip; Barry Teobald; Vince Russell

doi:10.1016/j.bmcl.2011.10.002

The discovery of AZD9164, a novel muscarinic M3 antagonist

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7440-6. doi: 10.1016/j.bmcl.2011.10.002. Epub 2011 Oct 8.

Authors

Antonio Mete¹, Keith Bowers, Eric Chevalier, David K Donald, Helen Edwards, Katherine J Escott, Rhonan Ford, Ken Grime, Ian Millichip, Barry Teobald, Vince Russell

Affiliation

¹ Department of Chemistry, AstraZeneca R&D Charnwood, Bakewell Road, Loughborough, Leicestershire LE11 5RH, UK. antonio.mete@astrazeneca.com

PMID: 22047691
DOI: 10.1016/j.bmcl.2011.10.002

Abstract

The optimization of a new series of muscarinic M(3) antagonists is described, leading to the identification of AZD9164 which was progressed into the clinic for evaluation of its potential as a treatment for COPD.

MeSH terms

Blood Proteins / metabolism
Drug Evaluation, Preclinical
Humans
Muscarinic Antagonists / chemistry*
Muscarinic Antagonists / pharmacology
Muscarinic Antagonists / therapeutic use
Piperidines / chemistry*
Piperidines / pharmacology
Piperidines / therapeutic use
Protein Binding
Pulmonary Disease, Chronic Obstructive / drug therapy
Quinuclidines / chemistry*
Quinuclidines / pharmacology
Quinuclidines / therapeutic use
Receptor, Muscarinic M3 / agonists*
Receptor, Muscarinic M3 / metabolism
Structure-Activity Relationship

Substances

AZD9164
Blood Proteins
Muscarinic Antagonists
Piperidines
Quinuclidines
Receptor, Muscarinic M3