Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists

Anandan Palani; Sundeep Dugar; John W Clader; William J Greenlee; Vilma Ruperto; Ruth A Duffy; Jean E Lachowicz

doi:10.1016/j.bmcl.2004.01.033

Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1791-4. doi: 10.1016/j.bmcl.2004.01.033.

Authors

Anandan Palani¹, Sundeep Dugar, John W Clader, William J Greenlee, Vilma Ruperto, Ruth A Duffy, Jean E Lachowicz

Affiliation

¹ Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. anandan.palani@spcorp.com

PMID: 15026073
DOI: 10.1016/j.bmcl.2004.01.033

Abstract

Low molecular weight amide derivatives were synthesized and evaluated as M(2) receptor antagonists for the treatment of Alzheimer's disease. Isopropyl amides 19 and 31 are highly potent, selective and low molecular weight M(2) receptor antagonists with structural features different from our clinical candidate 1.

MeSH terms

Amides / chemical synthesis*
Humans
Muscarinic Antagonists / chemical synthesis
Muscarinic Antagonists / chemistry*
Muscarinic Antagonists / metabolism*
Protein Binding / physiology
Receptor, Muscarinic M2 / antagonists & inhibitors*
Receptor, Muscarinic M2 / metabolism*

Substances

Amides
Muscarinic Antagonists
Receptor, Muscarinic M2