Synthesis and pharmacological properties of N-[3-(3-(1-Piperidinylmethyl)phenoxy)propyl]-2-(2-hydroxyethylthio)- acetamide and related compounds as antiulcer agents. I.
N-Phenoxypropylacetamide derivatives were prepared and tested for antiulcer activity. These compounds exhibited both gastric acid antisecretory and cytoprotective properties. Structure-activity studies led to the identification of N-[3-(3-(1-piperidinylmethyl)phenoxy)propyl]-2-(2-hydroxyethylt hio)acetamide (8), which was selected for further development and clinical evaluation.
Ueda
I
I
Institute of Scientific and Industrial Research, Osaka University, Japan.
Ishii
K
K
Shinozaki
K
K
Seiki
M
M
Arai
H
H
Hatanaka
M
M
D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis*; D004285:Dogs; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013853:Thioacetamide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000897:Anti-Ulcer Agents; D010880:Piperidines; D013853:Thioacetamide