6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists

  • Bioorg Med Chem Lett. 2009 Jun 1;19(11):3113-7. doi: 10.1016/j.bmcl.2009.03.166.
Lee R Roberts  1 ,  Paul V Fish ,  R Ian Storer ,  Gavin A Whitlock
Affiliations
  • 1. Department of Chemistry, Pfizer Global Research and Development, Sandwich Labs, Sandwich, Kent, UK. [email protected]
PMID: 19414260 DOI: 10.1016/j.bmcl.2009.03.166
Abstract

Novel pyrroloimidazoles 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 subtypes. Pyrimidine 19 possessed attractive CNS drug-like properties with good membrane permeability and no evidence for P-gp mediated efflux.