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

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

Affiliation

  • 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.

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