Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

Stephen D Goble; Liping Wang; K Lulu Howell; Alka Bansal; Richard Berger; Linda Brockunier; Jerry DiSalvo; Scott Feighner; Bart Harper; Jiafang He; Amanda Hurley; Donna Hreniuk; Emma Parmee; Michael Robbins; Gino Salituro; Anthony Sanfiz; Eric Streckfuss; Eloisa Watkins; Ann E Weber; Mary Struthers; Scott D Edmondson

doi:10.1016/j.bmcl.2010.01.130

Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. doi: 10.1016/j.bmcl.2010.01.130. Epub 2010 Feb 4.

Affiliation

¹ Merck Research Laboratories, Rahway, NJ 07065, USA. stephen_goble@merck.com

PMID: 20181479
DOI: 10.1016/j.bmcl.2010.01.130

Abstract

A series of amide derived beta(3)-adrenergic receptor (AR) agonists is described. The discovery and optimization of several series of compounds derived from 1, is used to lay the SAR foundation for second generation beta(3)-AR agonists for the treatment of overactive bladder.

MeSH terms

Acetamides / pharmacokinetics
Acetamides / pharmacology*
Adrenergic beta-3 Receptor Agonists*
Adrenergic beta-Antagonists / pharmacokinetics
Adrenergic beta-Antagonists / pharmacology*
Animals
Benzamides / pharmacokinetics
Benzamides / pharmacology*
Rodentia
Structure-Activity Relationship

Substances

Acetamides
Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Antagonists
Benzamides