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

…, T Kottke, X Ligneau, JC Camelin, JC Schwartz…

Index: Walter; Isensee; Kottke; Ligneau; Camelin; Schwartz; Stark Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 19 p. 5883 - 5886

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Citation Number: 5

Abstract

With a small series of compounds we demonstrated the variability in the core region of the human histamine H3 receptor (hH3R) 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.