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)a...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1990-11, Vol.38 (11), p.3035-3041
Hauptverfasser:	UEDA, I, ISHII, K, SHINOZAKI, K, SEIKI, M, ARAI, H, HATANAKA, M
Format:	Artikel
Sprache:	eng
Schlagworte:	Aliphatic compounds Animals Anti-Ulcer Agents - chemical synthesis Chemistry Dogs Exact sciences and technology Male Organic chemistry Piperidines - chemical synthesis Piperidines - pharmacology Preparations and properties Rats Rats, Inbred Strains Thioacetamide - analogs & derivatives Thioacetamide - chemical synthesis Thioacetamide - pharmacology
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Beschreibung
Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.38.3035