Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents
In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4...
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| Veröffentlicht in: | Pharmazie 2004-12, Vol.59 (12), p.899-905 |
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| container_title | Pharmazie |
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| creator | Shafik, R M El-Din, S A Shams Eshba, N H El-Hawash, S A M Desheesh, M A Abdel-Aty, A S Ashour, H M |
| description | In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4-tetrahydropyrimido[1,6-a]benzimidazoles 15 were synthesized. Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg). |
| format | Article |
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Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg).</description><identifier>ISSN: 0031-7144</identifier><identifier>PMID: 15638075</identifier><language>eng</language><publisher>Germany</publisher><subject>Animals ; Anti-Ulcer Agents - chemical synthesis ; Anti-Ulcer Agents - pharmacology ; Benzimidazoles - chemical synthesis ; Benzimidazoles - pharmacology ; Body Weight ; Gastric Mucosa - drug effects ; Gastric Mucosa - secretion ; Indicators and Reagents ; Male ; Omeprazole - pharmacology ; Pylorus - physiology ; Pyrimidines - chemical synthesis ; Pyrimidines - pharmacology ; Rats ; Structure-Activity Relationship</subject><ispartof>Pharmazie, 2004-12, Vol.59 (12), p.899-905</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15638075$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Shafik, R M</creatorcontrib><creatorcontrib>El-Din, S A Shams</creatorcontrib><creatorcontrib>Eshba, N H</creatorcontrib><creatorcontrib>El-Hawash, S A M</creatorcontrib><creatorcontrib>Desheesh, M A</creatorcontrib><creatorcontrib>Abdel-Aty, A S</creatorcontrib><creatorcontrib>Ashour, H M</creatorcontrib><title>Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents</title><title>Pharmazie</title><addtitle>Pharmazie</addtitle><description>In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4-tetrahydropyrimido[1,6-a]benzimidazoles 15 were synthesized. Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg).</description><subject>Animals</subject><subject>Anti-Ulcer Agents - chemical synthesis</subject><subject>Anti-Ulcer Agents - pharmacology</subject><subject>Benzimidazoles - chemical synthesis</subject><subject>Benzimidazoles - pharmacology</subject><subject>Body Weight</subject><subject>Gastric Mucosa - drug effects</subject><subject>Gastric Mucosa - secretion</subject><subject>Indicators and Reagents</subject><subject>Male</subject><subject>Omeprazole - pharmacology</subject><subject>Pylorus - physiology</subject><subject>Pyrimidines - chemical synthesis</subject><subject>Pyrimidines - pharmacology</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><issn>0031-7144</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkMtKw0AUhrNQbK2-gsxKFDIwt0xSXEnxBgUXdldKmGZOzMh0JmYmQvpGvqVR68bVgY__fIfzHyVTQjjFORVikpyG8EYIk0wWJ8mEZpIXJM-myefL4GIDwQTka-T8B1jE8Jrhq9BvQzSxj6CR2hnnr9sGHMRmsBtM0SPegtubndFq7y2EG8RTgbVpBt15pJxGNGXpyFIcIXbqh7dD973h1zSVWG3-KZAKqPURXDTKjopoeltBh9TriMJZclwrG-D8MGfJ6v5utXjEy-eHp8XtEreZyPC80hKKTBIiSC4I0Vxk81qAAAqaMA5aAS8KwkFUtKqkYppRUQups0oBKD5LLn-1beffewix3JlQgbXKge9DKXNGyHhgDF4cgv12B7psx9dUN5R_3fIvoVR2ag</recordid><startdate>200412</startdate><enddate>200412</enddate><creator>Shafik, R M</creator><creator>El-Din, S A Shams</creator><creator>Eshba, N H</creator><creator>El-Hawash, S A M</creator><creator>Desheesh, M A</creator><creator>Abdel-Aty, A S</creator><creator>Ashour, H M</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>200412</creationdate><title>Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents</title><author>Shafik, R M ; El-Din, S A Shams ; Eshba, N H ; El-Hawash, S A M ; Desheesh, M A ; Abdel-Aty, A S ; Ashour, H M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p545-9cd6e85600407400d3459f4e4e1ed023edae38803e4c1cc6a2d214f46d5caeea3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>Animals</topic><topic>Anti-Ulcer Agents - chemical synthesis</topic><topic>Anti-Ulcer Agents - pharmacology</topic><topic>Benzimidazoles - chemical synthesis</topic><topic>Benzimidazoles - pharmacology</topic><topic>Body Weight</topic><topic>Gastric Mucosa - drug effects</topic><topic>Gastric Mucosa - secretion</topic><topic>Indicators and Reagents</topic><topic>Male</topic><topic>Omeprazole - pharmacology</topic><topic>Pylorus - physiology</topic><topic>Pyrimidines - chemical synthesis</topic><topic>Pyrimidines - pharmacology</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Shafik, R M</creatorcontrib><creatorcontrib>El-Din, S A Shams</creatorcontrib><creatorcontrib>Eshba, N H</creatorcontrib><creatorcontrib>El-Hawash, S A M</creatorcontrib><creatorcontrib>Desheesh, M A</creatorcontrib><creatorcontrib>Abdel-Aty, A S</creatorcontrib><creatorcontrib>Ashour, H M</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmazie</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Shafik, R M</au><au>El-Din, S A Shams</au><au>Eshba, N H</au><au>El-Hawash, S A M</au><au>Desheesh, M A</au><au>Abdel-Aty, A S</au><au>Ashour, H M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents</atitle><jtitle>Pharmazie</jtitle><addtitle>Pharmazie</addtitle><date>2004-12</date><risdate>2004</risdate><volume>59</volume><issue>12</issue><spage>899</spage><epage>905</epage><pages>899-905</pages><issn>0031-7144</issn><abstract>In an effort to establish new antiulcer agents a series of 2-(2-substituted amino)-1 H-benzimidazoles 8, 9, 14; 1,3-disubstituted-3,4-dihydropyrimido[1,6-a]benzimidazoles 4, 7, 11, 12; 3-substituted-3,4-dihydropyrimido[1,6-a]benzimidazol-1 (2H)-thiones (or (2H)-ones) 10, 17 and 3-substituted-1,2,3,4-tetrahydropyrimido[1,6-a]benzimidazoles 15 were synthesized. Representative members were selected to evaluate their gastric antisecretory activity using an in vivo pylorus ligated rat method. Omeprazole was used as reference. The results indicated that the test compounds exhibit gastric antisecretory activity. The percent inhibition+/-SEM at the indicated dose level was demonstrated as omeprazole (59%+/-0.16 at 3 mg/kg) > 15a (53%+/-1.39 at 3 mg/kg) > 7a (51%+/-1.04 at 1 mg/kg) > 10a (50%+/-1.36 at 3 mg/kg).</abstract><cop>Germany</cop><pmid>15638075</pmid><tpages>7</tpages></addata></record> |
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| language | eng |
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| source | MEDLINE; IngentaConnect Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Animals Anti-Ulcer Agents - chemical synthesis Anti-Ulcer Agents - pharmacology Benzimidazoles - chemical synthesis Benzimidazoles - pharmacology Body Weight Gastric Mucosa - drug effects Gastric Mucosa - secretion Indicators and Reagents Male Omeprazole - pharmacology Pylorus - physiology Pyrimidines - chemical synthesis Pyrimidines - pharmacology Rats Structure-Activity Relationship |
| title | Synthesis of novel 2-[2-(substituted amino)phenethyl]-1 H-benzimidazoles; 3,4-dihydro and 1,2,3,4,-tetrahydropyrimido[1,6-a]-benzimidazoles as potential antiulcer agents |
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