Medicinal chemical and pharmacological aspects of imidazole-containing histamine H3 receptor antagonists.
The first antagonists known for the histamine H3 receptor were mono-substituted imidazole-containing compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.
Stark
Holger
H
Johann Wolfgang Goethe-Universität, Institut für Pharmazeutische Chemie, Biozentrum, Marie-Curie-Strasse 9, 60439 Frankfurt am Main, Germany. h.stark@pharmchem.uni-frankfurt.de.
Kathmann
Markus
M
Schlicker
Eberhard
E
Schunack
Walter
W
Schlegel
Birgit
B
Sippl
Wolfgang
W
D000818:Animals; D006633:Histamine Antagonists / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D008024:Ligands; D021281:Quantitative Structure-Activity Relationship; D018100:Receptors, Histamine H3 / Q000737:chemistry / Q000378:metabolism*
D006633:Histamine Antagonists; D007093:Imidazoles; D008024:Ligands; D018100:Receptors, Histamine H3; C029899:imidazole