Novel 2-imidazoles as potent and selective alpha1A adrenoceptor partial agonists

  • Bioorg Med Chem Lett. 2008 May 1;18(9):2930-4. doi: 10.1016/j.bmcl.2008.03.070.
Gavin A Whitlock  1 ,  Kelly Conlon ,  Gordon McMurray ,  Lee R Roberts ,  Alan Stobie ,  Richard J Thurlow
Affiliations
  • 1. Department of Chemistry, Pfizer Global Research and Development, Sandwich Labs, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. [email protected]
PMID: 18400496 DOI: 10.1016/j.bmcl.2008.03.070
Abstract

Novel 2-imidazoles have been identified as potent partial agonists of the alpha(1A) Adrenergic Receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Sulfonamide 23 possessed attractive drug-like properties with respect to physicochemical and ADME properties and wide ligand selectivity.