Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.
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.
Walter
M
M
Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biocenter, ZAFES/LiFF/CMP/ICNF, Max-von-Laue-Str 9, 60438 Frankfurt, Germany.
von Coburg
Y
Y
Isensee
K
K
Sander
K
K
Ligneau
X
X
Camelin
J-C
JC
Schwartz
J-C
JC
Stark
H
H
D001393:Azoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004987:Ethers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D054828:Histamine H3 Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D018100:Receptors, Histamine H3 / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*
D001393:Azoles; D004987:Ethers; D054828:Histamine H3 Antagonists; D018100:Receptors, Histamine H3; D013844:Thiazoles