Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers

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

doi:10.1016/j.bmcl.2010.07.098

Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5879-82. doi: 10.1016/j.bmcl.2010.07.098. Epub 2010 Aug 1.

Authors

M Walter¹, Y von Coburg, K Isensee, K Sander, X Ligneau, J-C Camelin, J-C Schwartz, H Stark

Affiliation

¹ Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biocenter, ZAFES/LiFF/CMP/ICNF, Max-von-Laue-Str 9, 60438 Frankfurt, Germany.

PMID: 20728354
DOI: 10.1016/j.bmcl.2010.07.098

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Azoles / chemical synthesis
Azoles / chemistry*
Azoles / pharmacology
Cell Line
Ethers / chemical synthesis
Ethers / chemistry*
Ethers / pharmacology
Histamine H3 Antagonists / chemical synthesis
Histamine H3 Antagonists / chemistry*
Histamine H3 Antagonists / pharmacology
Humans
Receptors, Histamine H3 / chemistry*
Receptors, Histamine H3 / metabolism
Structure-Activity Relationship
Thiazoles / chemistry*

Substances

Azoles
Ethers
Histamine H3 Antagonists
Receptors, Histamine H3
Thiazoles