Bioorganic and Medicinal Chemistry Letters p. 6577 - 6581 (2011)
Update date:2022-07-29
Topics:
Savall, Brad M.
Gomez, Laurent
Chavez, Frank
Curtis, Michael
Meduna, Steven P.
Kearney, Aaron
Dunford, Paul
Cowden, Jeffery
Thurmond, Robin L.
Grice, Cheryl
Edwards, James P.
This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
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