期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 21, 页码 6577-6581出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.014
关键词
Histamine; Histamine H4; Antagonists; Benzofuran; Amino pyrimidine; Tricyclic
This report discloses the development of a series of tricyclic histamine H-4 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 H-4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model. (C) 2011 Elsevier Ltd. All rights reserved.
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