Quinoxaline chemistry. Part 6--Synthesis and evaluation of antiulcer and gastroprotective activity of 2-[arylmethylmercapto-, arylmethylsulfinyl-, piperazinyl-3-R-substituted]quinoxalines.
Thirty compounds possessing quinoxaline structure bearing either substituted arylmethylmercapto-, arylmethylsulfinyl group or a piperazinyl moiety in position 2 were prepared in order to evaluate an antiulcer and gastroprotective activity in rat pylorus ligature, in comparison with omeprazole and ranitidine at the dose of 100 mg/kg after oral administration. Among the compounds of the first group one third showed a moderate activity being about half potent as omeprazole whereas in the second group compound 5b exibited an activity superior to that of ranitidine accompanied with the lowest incidence of lesions and mortality and another compound (5i) was equiactive as ranitidine.
Piras
S
S
Istituto di Chimica Farmaceutica e Tossicologica dell'Università di Sassari, Muroni.
Loriga
M
M
Paglietti
G
G
Demontis
M P
MP
Varoni
M V
MV
Fattaccio
M C
MC
Anania
V
V
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D005753:Gastric Mucosa / Q000187:drug effects*; D008297:Male; D009853:Omeprazole / Q000494:pharmacology; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology; D011899:Ranitidine / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D011810:Quinoxalines; D011899:Ranitidine; D009853:Omeprazole