[Studies on the synthesis of antiulcer agents. VII. Synthesis and antiulcer activity of dihydrobenzofuranone derivatives].
A number of 2-substituted 2,3-dihydro-3-oxo-5-benzofuranylacryloyl derivatives were synthesized and tested for antiulcer activities in order to study structure-activity relationships. Significant antiulcer activities were found in only the compounds (2e-g, p, s) in which hydroxymethyl and methyl groups or acetoxymethyl and methyl groups were introduced on the 2-position of the benzofuranone skeleton. Among the compounds tested, 1-[3-(2,3-dihydro-2-hydroxymethyl-2-methyl-3-oxo-5-benzofuranyl)acryloyl ] piperidine (2e) was the most promising compound.
Kitazawa
M
M
Akahane
M
M
Nakano
Y
Y
Hayakawa
K
K
Sato
K
K
Kobayashi
M
M
D000179:Acrylates / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000897:Anti-Ulcer Agents; D001572:Benzofurans / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000179:Acrylates; D000897:Anti-Ulcer Agents; D001572:Benzofurans