Studies on 2-Benzimidazolethiol Derivatives. V : Structure-Activity Relationship on Analgesic Action of 1-(Dialkylaminoalkyl)-2-(p-ethoxyphenylthio)benzimidazole

1-(2-Diethylaminoethyl)-2-(p-ethoxyphenylthio)benzimidazole (I) is considered to be a morphine-like analgesic and its derivatives, 1-(diethylaminoalkyl)-2-(p-ethoxyphenylthio) benzimidazoles, were synthesized to test their analgesic effect by the pressure method. Except for the 1-(2-pyrrolidinoethyl...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:YAKUGAKU ZASSHI 1967/03/25, Vol.87(3), pp.301-309
1. Verfasser: Seki, Teruya
Format: Artikel
Sprache:eng ; jpn
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:1-(2-Diethylaminoethyl)-2-(p-ethoxyphenylthio)benzimidazole (I) is considered to be a morphine-like analgesic and its derivatives, 1-(diethylaminoalkyl)-2-(p-ethoxyphenylthio) benzimidazoles, were synthesized to test their analgesic effect by the pressure method. Except for the 1-(2-pyrrolidinoethyl)derivative showing better activities than I or morphine, other derivatives did not show much effect, such as 1-diethylaminomethyl, 3-diethylaminopropyl, 1-[2-(allylamino)ethyl], 1-(2-dialkylaminopropyl), and 1-(1-methyl-2-piperidinoethyl) derivatives. The allyl derivative did not show any antagonistic action against I or morphine. Some discussions were made on the central atom, basic nitrogen, and the flat aromatic portion in the molecules of I and its analogs.
ISSN:0031-6903
1347-5231
DOI:10.1248/yakushi1947.87.3_301