Tricyclic aminopyrimidine histamine H 4 receptor antagonists

…, SP Meduna, A Kearney, P Dunford, J Cowden…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 21 p. 6577 - 6581

全文：HTML全文

被引用次数: 20

摘要

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.