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

作者：Walter M; von Coburg Y; Isensee K; Sander K; Ligneau X; Camelin J C; Schwartz J C; Stark H^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(19): 5879-5882.

DOI：10.1016/j.bmcl.2010.07.098

• GPCR
• Histamine
• H3
• Pharmacophore

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.

• 出版日期2010-10-1