The solid state structure of the Rimazolium hydroxylation product I was determined by X-ray investigations, and stereostructure of 1,6,7,8,9,9a-hexahydro-4H-pyrido[1,2-a]pyrimidin-4-ones were studied by semiempirical quantum chem. calculations at the AM1 level.While 9a-unsubstituted 1-methyl-1,6,7,8,9,9a-hexahydro-4H-pyrido[1,2-a]pyrimidin-4-ones adopt a cis-fused conformation, I has a trans-fused conformation to avoid a serious non-bonding interaction between the 9a-ethoxy and 1-Me groups.

01 Jan 1992·Acta physiologica Hungarica

The mechanism of cytoprotective effect of CHINOIN-127.

Article

Author: Hermecz, I ; Kapui, Z ; Boér, K ; Gyíres, K

According earlier, investigations nitrogen bridgehead compounds make a representative group of non-prostaglandin type gastroprotective agents. One member of this group is CHINOIN-127 (1,6-dimethyl-4-oxo-1, 6, 7, 8, 9, 9a-hexahydro-4H-pyrido-(1, 2a)-pyrimidine-3-carbox-amide). CHINOIN-127 is a potent non-narcotic analgesic and antiinflammatory agent and has a remarkable protective effect on indomethacin induced ulcer (ED50 = 25 mg/kg p.o.) and on acidified ethanol induced ulcer (ED50 = 26 mg/kg p.o.). In this study we examined the mechanism of action of cytoprotective effect of this drug and we made a comparison between the cytoprotective effect of 20% ethanol and 25 mg/kg CHINOIN-127. In the gastric mucosa of control rats we observed a balance between TxA2 and PGI2 (PGI2/TxA2 = 3.8) and between the cytoprotective prostaglandins (PGI2 and PGE2) and ulcerogen eicosanoids (TxA2 and leukotrienes) (PGI2 + PGE2/TxA2 + LTs = 3.9). 100% ethanol treatment causes disintegration of this balance, shifting the synthesis towards the ulcerogen eicosanoids production. CHINOIN-127 and 20% ethanol pretreatment improves the deranged balance between cytoprotective prostaglandins and ulcerogen eicosanoids. Our results demonstrate that CHINOIN-127 and 20% ethanol have a similar mechanism of cytoprotective action on ethanol induced ulcer in rats.

01 Jan 1990·Acta physiologica Hungarica

The gastroprotective effect of CHINOIN-127 on indomethacin induced gastric ulcer in rats.

Article

Author: Kapui, Z ; Kovács, Z ; Hermecz, I ; Cser, I ; Blaskó, G ; Rózsa, I

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Indication	Highest Phase	Country/Location	Organization	Date
Peptic Ulcer	Preclinical	Hungary	Chinoin Zrt.	-

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