2. Academic Validation
  3. Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules

Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1354-8. doi: 10.1016/j.bmcl.2011.01.043.
Adam D Hughes 1,  Kay H Chin,  Sarah L Dunham,  Jeffrey R Jasper,  Kristin E King,  Tae Weon Lee,  Mathai Mammen,  Jerri Martin,  Tod Steinfeld
Affiliations

Affiliation

  • 1 Theravance, Inc., South San Francisco, CA 94080, USA. ahughes@theravance.com
PMID: 21310610 DOI: 10.1016/j.bmcl.2011.01.043
Abstract

We sought to design dual pharmacology bronchodilators targeting both the M(3) muscarinic acetylcholine and beta-2 adrenergic (β(2)) receptors by applying our multivalent approach to drug discovery. Herein, we describe our initial discovery and the SAR of the first such compounds with matched potencies at both receptors.

Figures