Synthesis and evaluation of gastroprotective activity of omeprazole related benzimidazole, imidazo[4,5-b]pyridine and quinoxaline 2-substituted derivatives.
Twenty compounds possessing benzimidazole, imidazo[4,5-b]pyridine and quinoxaline structure bearing either a substituted arylmethylmercapto- or an arylmethylsulfinyl group in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole at the dose of 50 mg/kg after i.m. administration. One third of these compounds showed a moderate activity, being about half potent as omeprazole.
Piras
S
S
Istituto di Chimica Farmaceutica e'Tossicologica dell'Università di Sassari.
Loriga
M
M
Paglietti
G
G
Sparatore
F
F
Demontis
M P
MP
Varoni
M V
MV
Fattaccio
M C
MC
Anania
V
V
D000818:Animals; D000897:Anti-Ulcer Agents / Q000737:chemistry* / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D009853:Omeprazole / Q000494:pharmacology*; D011687:Purines / Q000737:chemistry / Q000494:pharmacology*; D011708:Pylorus / Q000187:drug effects; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D011687:Purines; D011810:Quinoxalines; C064191:1H-imidazo(4,5-b)pyridine; C031000:benzimidazole; D009853:Omeprazole