Azole derivatives as histamine H 3 receptor antagonists, Part I: Thiazol-2-yl ethers

…, Y Von Coburg, K Isensee, K Sander, X Ligneau…

Index: Walter; Von Coburg; Isensee; Sander; Ligneau; Camelin; Schwartz; Stark Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5879 - 5882

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Citation Number: 7

Abstract

Most human histamine H3 receptor (hH3R) antagonists follow a general structural blueprint, containing a basic moiety linked by a spacer to a substituted core element. In this investigation the acceptance of thiazol-2-yl ether moieties in the core region is proved with some ether derivatives showing hH3R binding affinities in the nanomolar concentration range. A diversity of structural motifs is used as substituents to enhance the in vitro hH3R ...