Condensed thienopyrimidines. I. Synthesis and gastric antisecretory activity of 2,3-dihydro-5H-oxazolothienopyrimidin-5-one derivatives.
A practical preparation of various 2,3-dihydro-5H-oxazolo[3,2-a]thieno[3,2-d]-, [3,4-d]-, and [2,3-d]pyrimidin-5-one derivatives was developed starting from the corresponding aminothiopheneesters in two steps, and their chloro-substituted derivatives were prepared. These compounds were evaluated for gastric antisecretory activity in pylorus-ligated rats, compared to the anti-ulcer standard, cimetidine, and their structure-activity relationships are discussed.
Sugiyama
M
M
Sakamoto
T
T
Tabata
K
K
Endo
K
K
Ito
K
K
Kobayashi
M
M
Fukumi
H
H
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D008297:Male; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D011744:Pyrimidinones; C062125:2,3-dihydro-5H-oxazolothienopyrimidin-5-one