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...
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Veröffentlicht in: | YAKUGAKU ZASSHI 1967/03/25, Vol.87(3), pp.301-309 |
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description | 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. |
doi_str_mv | 10.1248/yakushi1947.87.3_301 |
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V : Structure-Activity Relationship on Analgesic Action of 1-(Dialkylaminoalkyl)-2-(p-ethoxyphenylthio)benzimidazole</title><source>MEDLINE</source><source>J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese</source><source>Alma/SFX Local Collection</source><creator>Seki, Teruya</creator><creatorcontrib>Seki, Teruya</creatorcontrib><description>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. 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Some discussions were made on the central atom, basic nitrogen, and the flat aromatic portion in the molecules of I and its analogs.</description><subject>Analgesics - pharmacology</subject><subject>Benzimidazoles - pharmacology</subject><subject>Chemical Phenomena</subject><subject>Chemistry</subject><subject>Chromatography</subject><subject>Spectrum Analysis</subject><issn>0031-6903</issn><issn>1347-5231</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1967</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNplUcFu1DAQtRCorEr_AKScUHvwYsdO7HBbWihIlZAocLUce9I1deLUTirSv-FPSbrLqhJzmdF7b96M9BB6Tcma5ly-m_TtmLaOVlyspVgzxQh9hlaUcYGLnNHnaEUIo7isCHuJTlJyNSH5XAWVR-ioJGXFRLlCf66H0TpIWeiyHH-A7sG1zuqH4GHYuuCzC4juXg_uHtI6-5m9z66HOJphjIA3ZobdMGXfwM-K0M0P9YvRptP-BpIz2SKZgdBkFJ9eOO1vJ69b14XH6Qzn-LTH86Xwe-q30E1-OXpWP33jFXrRaJ_gZN-P0Y9PH7-ff8ZXXy-_nG-usGG5oFjb0kjQZU2sEboUkjaiMKy2TWELsHkuG20bXTU11EXNRcmNqXhupW6KBWHH6O3Ot4_hboQ0qNYlA97rDsKYlORFQbnks5DvhCaGlCI0qo-u1XFSlKglHPUkHCWFegxnXnuz9x_rFuxhaR_FzF_u-F9p0Ddw4HUcnPHwv-k_54PCbHVU0LG_LoOrxA</recordid><startdate>196703</startdate><enddate>196703</enddate><creator>Seki, Teruya</creator><general>The Pharmaceutical Society of Japan</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>196703</creationdate><title>Studies on 2-Benzimidazolethiol Derivatives. 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V : Structure-Activity Relationship on Analgesic Action of 1-(Dialkylaminoalkyl)-2-(p-ethoxyphenylthio)benzimidazole</atitle><jtitle>YAKUGAKU ZASSHI</jtitle><addtitle>YAKUGAKU ZASSHI</addtitle><date>1967-03</date><risdate>1967</risdate><volume>87</volume><issue>3</issue><spage>301</spage><epage>309</epage><pages>301-309</pages><issn>0031-6903</issn><eissn>1347-5231</eissn><abstract>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.</abstract><cop>Japan</cop><pub>The Pharmaceutical Society of Japan</pub><pmid>6069376</pmid><doi>10.1248/yakushi1947.87.3_301</doi><tpages>9</tpages><oa>free_for_read</oa></addata></record> |
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language | eng ; jpn |
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source | MEDLINE; J-STAGE (Japan Science & Technology Information Aggregator, Electronic) Freely Available Titles - Japanese; Alma/SFX Local Collection |
subjects | Analgesics - pharmacology Benzimidazoles - pharmacology Chemical Phenomena Chemistry Chromatography Spectrum Analysis |
title | Studies on 2-Benzimidazolethiol Derivatives. V : Structure-Activity Relationship on Analgesic Action of 1-(Dialkylaminoalkyl)-2-(p-ethoxyphenylthio)benzimidazole |
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