Azole derivatives as histamine H3 receptor antagonists, Part I: Thiazol-2-yl ethers

✍ Scribed by M. Walter; Y. von Coburg; K. Isensee; K. Sander; X. Ligneau; J.-C. Camelin; J.-C. Schwartz; H. Stark

• Book ID: 104004698
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 829 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.07.098

✦ Synopsis

Most human histamine H 3 receptor (hH 3 R) 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 hH 3 R binding affinities in the nanomolar concentration range. A diversity of structural motifs is used as substituents to enhance the in vitro hH 3 R binding affinity.