Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
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.
Beaulieu
Christian
C
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Kirkland, QC, Canada H9R 4P8. christian_beaulieu@merck.com
Wang
Zhaoyin
Z
Denis
Danielle
D
Greig
Gillian
G
Lamontagne
Sonia
S
O'Neill
Gary
G
Slipetz
Deborah
D
Wang
Jennifer
J
D018926:Anti-Allergic Agents / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D001562:Benzimidazoles / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D001667:Binding, Competitive / Q000187:drug effects; D006801:Humans; D011485:Protein Binding / Q000187:drug effects; D011869:Radioligand Assay; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012221:Rhinitis, Allergic, Perennial / Q000188:drug therapy* / Q000378:metabolism
D018926:Anti-Allergic Agents; D001562:Benzimidazoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor