Novel imidazo[1,2-a]pyrazine derivatives as potent reversible inhibitors of the gastric H+/K+-ATPase.
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.
Zimmermann
Peter Jan
PJ
Nycomed GmbH, Byk-Gulden-Str. 2, D-78467 Konstanz, Germany. pjz@lycos.de
Brehm
Christof
C
Buhr
Wilm
W
Palmer
Andreas Marc
AM
Volz
Jürgen
J
Simon
Wolfgang-Alexander
WA
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
D004791:Enzyme Inhibitors; D054328:Proton Pump Inhibitors; D011719:Pyrazines