Synthesis and gastroprotective activity of 4H-pyrido[1,2-a]pyrimidin-4-ones.
The cytoprotective effect of different types of 4h-pyrido[1,2-a]pyrimidin-4-one derivatives was investigated. Short synthesis of the investigated compounds was depicted. The gastroprotective effect was determined against acidified ethanol induced mucosal lesions in rats. The most effective compounds belong to unsaturated 4-oxo-4h-pyrido[1,2-a]pyrimidine-3-carboxamide derivatives, and the most active one contains a methyl group in position 6 and a cyclopentyl group on the nitrogen of the carboxamide group. Further pharmacological, biochemical and clinical studies may justify, that the representative of this type of compounds may be useful as prophylactic agents against gastric damage caused by non-steroidal antiinflammatory agents.
Hermecz
I
I
Chinoin Pharmaceutical and Chemical Works Ltd., Budapest, Hungary.
Sipos
J
J
Vasvári-Debreczy
L
L
Gyires
K
K
Kapui
Z
Z
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001285:Atropine / Q000494:pharmacology; D002927:Cimetidine / Q000494:pharmacology; D003663:Decision Trees; D000431:Ethanol; D007213:Indomethacin; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013276:Stomach Ulcer / Q000139:chemically induced / Q000473:pathology / Q000517:prevention & control*; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D011744:Pyrimidinones; D000431:Ethanol; D001285:Atropine; D002927:Cimetidine; D007213:Indomethacin