title: Novel imidazo[1,2-a]pyrazine derivatives as potent reversible inhibitors of the gastric H+/K+-ATPase.
abstract: A series of novel 6-substituted imidazo[1,2-a]pyrazines were synthesized via palladium catalyzed amino- or alkoxycarbonylation as key step. The anti-secretory activity of these compounds has been assessed in a binding assay against H(+)/K(+)-ATPase from hog gastric mucosa. Some of the compounds proved to be potent inhibitors of the gastric acid pump.
authors.affiliation: Nycomed GmbH, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany. pjz@lycos.de
authors.forename: Peter Jan
authors.initials: PJ
authors.lastname: Zimmermann
authors.forename: Christof
authors.initials: C
authors.lastname: Brehm
authors.forename: Wilm
authors.initials: W
authors.lastname: Buhr
authors.forename: Andreas Marc
authors.initials: AM
authors.lastname: Palmer
authors.forename: Jürgen
authors.initials: J
authors.lastname: Volz
authors.forename: Wolfgang-Alexander
authors.initials: WA
authors.lastname: Simon
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D054328:Proton Pump Inhibitors; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013270:Stomach / Q000201:enzymology*; D013552:Swine
chemical_list: D004791:Enzyme Inhibitors; D054328:Proton Pump Inhibitors; D011719:Pyrazines