Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.

Bioorg Med Chem Lett

Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biozentrum, ZAFES/LiFF/CMP/ICNF, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.

Published: October 2010

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Article Abstract

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.

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http://dx.doi.org/10.1016/j.bmcl.2010.07.109DOI Listing

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