Azole derivatives as histamine H-3 receptor antagonists, Part 2: C-C and C-S coupled heterocycles

作者：Walter M; Isensee K; Kottke T; Ligneau X; Camelin J C; Schwartz J C; Stark H^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(19): 5883-5886.

DOI：10.1016/j.bmcl.2010.07.109

• GPCR
• Histamine
• H3
• Pharmacophore
• Medicinal chemistry
• Bioisosteric replacement

With a small series of compounds we demonstrated the variability in the core region of the human histamine H-3 receptor (hH(3)R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Additional variations achieved by coupling different residues to the heterocyclic core structure led to further optimisation of in vitro receptor binding of the novel azole derivatives.

• 出版日期2010-10-1