Synthesis and evaluation of gastroprotective and antiulcer activity of some 2-substituted-1H-imidazo[4,5-b] pyridines and -1H-benzimidazoles.
Several compounds possessing imidazo[4,5-b]pyridine and benzimidazole structure bearing substituents in position 2 were prepared in order to evaluate an anti-ulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole. Among sixteen compounds taken as representatives of the synthetised series only one (3d) showed a good activity by i.m. administration at 50 mg/kg, while by oral administration of 100 mg/kg a certain number was active and in some cases this activity was quite superior to that of omeprazole.
Loriga
M
M
Istituto di Chimica Farmaceutica e Tossicologica, Università di Sassari.
Paglietti
G
G
Piras
S
S
Sparatore
F
F
Anania
V
V
Demontis
M P
MP
Varoni
M V
MV
Fattaccio
M C
MC
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D004285:Dogs; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D009853:Omeprazole / Q000494:pharmacology; D011708:Pylorus / Q000502:physiology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013270:Stomach / Q000187:drug effects*
D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D007093:Imidazoles; D011725:Pyridines; D009853:Omeprazole