Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5451-5. doi: 10.1016/j.bmcl.2008.09.033.
David L Carlton  1 ,  Lissa J Collin-Smith ,  Alejandro J Daniels ,  David N Deaton ,  Aaron S Goetz ,  Christopher P Laudeman ,  Thomas R Littleton ,  David L Musso ,  Ronda J Ott Morgan ,  Jerzy R Szewczyk ,  Cunyu Zhang
Affiliations
  • 1. Department of Pharmaceutical Development, Physical Properties and Developability, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
PMID: 18818070 DOI: 10.1016/j.bmcl.2008.09.033
Abstract

Starting from a weak omeprazole screening hit, replacement of the pyridine with a 1,3-benzodioxole moiety, modification of the thioether linkage, and substitution of the benzimidazole pharmacophore led to the discovery of nanomolar BRS-3 agonists.