Synthesis and Cytoprotective Antiulcer Activity of 2- or 4-(1H-Pyrazol-1-yl)pyrimidine Derivatives Related to Mepirizole and Dulcerozine

(1H-Pyrazol-1-yl)-, (1H-imidazol-1-yl)-, and (1H-1, 2, 4-triazol-1-yl)phrimidines were prepared and evaluated for cytoprotective antiulcer activity. Among them, 4-methoxy-6-methyl-2-(1H-pyrazol-1-yl)pyrimidine (18) showed potent inhibition of the HCl-ethanol-induced and water-immersion stress-induce...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1996/09/15, Vol.44(9), pp.1700-1706
Hauptverfasser:	IKEDA, Masazumi, MARUYAMA, Kazumi, NOBUHARA, Youichi, YAMADA, Toshihiro, OKABE, Susumu
Format:	Artikel
Sprache:	eng
Schlagworte:	2-(1H-pyrazol-1-yl)pyrimidine Administration, Oral Animals Anti-Ulcer Agents - chemical synthesis Anti-Ulcer Agents - chemistry Anti-Ulcer Agents - therapeutic use Biological and medical sciences cytoprotective antiulcer activity Digestive system Disease Models, Animal dulcerozine Epirizole - chemistry Epirizole - pharmacology Magnetic Resonance Spectroscopy Male Medical sciences mepirizole Peptic Ulcer - drug therapy Pharmacology. Drug treatments Pyrimidines - chemistry Pyrimidines - pharmacology Rats Rats, Sprague-Dawley Structure-Activity Relationship
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Zusammenfassung:	(1H-Pyrazol-1-yl)-, (1H-imidazol-1-yl)-, and (1H-1, 2, 4-triazol-1-yl)phrimidines were prepared and evaluated for cytoprotective antiulcer activity. Among them, 4-methoxy-6-methyl-2-(1H-pyrazol-1-yl)pyrimidine (18) showed potent inhibition of the HCl-ethanol-induced and water-immersion stress-induced ulcers in rats, as well as low acute toxicity.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.44.1700