Studies on antiulcer drugs. V. Synthesis and antiulcer activity of aralkylbenzazoles.
A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagonist activity in contrast to imidazo[1,2-a]pyridine analogues (I). On antiulcer assay, however, some pyridine derivatives (II) exerted higher activity than the reference compounds, sofalcone, sucralfate and cimetidine. The structure-activity relationships of these compounds are discussed.
Katsura
Y
Y
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Inoue
Y
Y
Tomoi
M
M
Takasugi
H
H
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D006168:Guinea Pigs; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D051381:Rats; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D001562:Benzimidazoles; D001583:Benzoxazoles; D006635:Histamine H2 Antagonists; D013844:Thiazoles