Novel indanyl-substituted imidazo[1,2-a]pyridines as potent reversible inhibitors of the gastric H+/K+-ATPase.
A series of novel 8-indanylamino- and 8-indanyloxy-substituted imidazo[1,2-a]pyridines with reduced lipophilicity was synthesized from easily accessible starting compounds. The anti-secretory activity of these compounds has been assessed in a competitive 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
Buhr
Wilm
W
Brehm
Christof
C
Palmer
Andreas Marc
AM
Feth
Martin Philipp
MP
Senn-Bilfinger
Jörg
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 / Q000201:enzymology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D054328:Proton Pump Inhibitors; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013237:Stereoisomerism; D013270:Stomach / Q000187:drug effects / Q000201:enzymology*; D013329:Structure-Activity Relationship; D013552:Swine
D004791:Enzyme Inhibitors; D007093:Imidazoles; D007202:Indicators and Reagents; D054328:Proton Pump Inhibitors; D011725:Pyridines