A novel series of histamine H 4 receptor antagonists based on the pyrido [3, 2-d] pyrimidine scaffold: Comparison of hERG binding and target residence time with PF- …

M Andaloussi, HD Lim, T van der Meer, M Sijm…

文献索引：Andaloussi, Mounir; Lim, Herman D.; Van Der Meer, Tiffany; Sijm, Maarten; Poulie, Chris B.M.; De Esch, Iwan J.P.; Leurs, Rob; Smits, Rogier A. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 9 p. 2663 - 2670

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被引用次数: 14

摘要

In this work we describe the optimization of a lead compound based on the quinazoline template to give a new series of potent pyrido [3, 2-d] pyrimidines as histamine H4 receptor antagonists. The pyrido [3, 2-d] pyrimidine ligands have significantly reduced hERG binding compared to clinical stage compound PF-3893787 while showing good affinities at the human and rodent histamine receptors. The receptor residence time of several of these ...