Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis

Christian Beaulieu; Zhaoyin Wang; Danielle Denis; Gillian Greig; Sonia Lamontagne; Gary O'Neill; Deborah Slipetz; Jennifer Wang

doi:10.1016/j.bmcl.2004.04.005

Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3195-9. doi: 10.1016/j.bmcl.2004.04.005.

Authors

Christian Beaulieu¹, Zhaoyin Wang, Danielle Denis, Gillian Greig, Sonia Lamontagne, Gary O'Neill, Deborah Slipetz, Jennifer Wang

Affiliation

¹ Merck Frosst Centre for Therapeutic Research, PO Box 1005, Kirkland, QC, Canada H9R 4P8. christian_beaulieu@merck.com

PMID: 15149674
DOI: 10.1016/j.bmcl.2004.04.005

Abstract

A series of 2-substituted N-benzyl benzimidazole containing molecules has been synthesized and its structure-activity relationship for the human DP receptor has been evaluated. Selective DP antagonists with nanomolar potency for the DP receptor were identified in this novel series of benzimidazoles.

MeSH terms

Anti-Allergic Agents / chemistry*
Anti-Allergic Agents / metabolism
Anti-Allergic Agents / therapeutic use
Benzimidazoles / chemistry*
Benzimidazoles / metabolism
Benzimidazoles / therapeutic use
Binding, Competitive / drug effects
Humans
Protein Binding / drug effects
Radioligand Assay
Receptors, Immunologic
Receptors, Prostaglandin / antagonists & inhibitors*
Receptors, Prostaglandin / metabolism
Rhinitis, Allergic, Perennial / drug therapy*
Rhinitis, Allergic, Perennial / metabolism

Substances

Anti-Allergic Agents
Benzimidazoles
Receptors, Immunologic
Receptors, Prostaglandin
prostaglandin D2 receptor