title: First metal-containing histamine H3 receptor ligands.
abstract: Iron-containing ligands targeting the human histamine H(3) receptor (hH(3)R) were prepared. The compounds contain ferrocene sandwich complexes coupled via different linkers to a basic hH(3)R antagonist/inverse agonist pharmacophore. In a click chemistry approach, a triazole was successfully inserted as a new linking element. Two ferrocenylmethylamines and a ferrocenyltriazole were the most affine hH(3)R ligands within this series, showing receptor binding in the nano- and subnanomolar concentration range.
authors.affiliation: Johann Wolfgang Goethe University, Institute of Pharmaceutical Chemistry, Biocenter, Max-von-Laue-Strasse 9, 60438 Frankfurt am Main, Germany.
authors.forename: Kerstin
authors.initials: K
authors.lastname: Sander
authors.forename: Tim
authors.initials: T
authors.lastname: Kottke
authors.forename: Claas
authors.initials: C
authors.lastname: Hoffend
authors.forename: Miriam
authors.initials: M
authors.lastname: Walter
authors.forename: Lilia
authors.initials: L
authors.lastname: Weizel
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Camelin
authors.forename: Xavier
authors.initials: X
authors.lastname: Ligneau
authors.forename: Erich H
authors.initials: EH
authors.lastname: Schneider
authors.forename: Roland
authors.initials: R
authors.lastname: Seifert
authors.forename: Jean-Charles
authors.initials: JC
authors.lastname: Schwartz
authors.forename: Holger
authors.initials: H
authors.lastname: Stark
mesh_terms: D005296:Ferrous Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006633:Histamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D000075163:Metallocenes; D015394:Molecular Structure; D018100:Receptors, Histamine H3 / Q000187:drug effects / Q000378:metabolism*; D014230:Triazoles / Q000737:chemistry
chemical_list: D005296:Ferrous Compounds; D006633:Histamine Antagonists; D008024:Ligands; D000075163:Metallocenes; D018100:Receptors, Histamine H3; D014230:Triazoles; C004998:ferrocene