Novel N-[1-(1-substituted 4-piperidinylmethyl)-4piperidinyl]benzamides as potent colonic prokinetic agents
A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT(4) receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-ch...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2002-03, Vol.12 (6), p.967-970 |
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| container_end_page | 970 |
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| container_issue | 6 |
| container_start_page | 967 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 12 |
| creator | HARADA, Hiroshi YAMAZAKI, Hiroshi TOYOTOMI, Yoshihito TATEISHI, Hirotaka MINE, Yukiko YOSHIDA, Naoyuki KATO, Shiro |
| description | A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT(4) receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-chloro-2-methoxybenzamide (15) was found to have a potent binding affinity for 5-HT(4) receptors (IC(50): 6.47nM) and showed excellent colonic prokinetic activity. |
| doi_str_mv | 10.1016/S0960-894X(02)00060-4 |
| format | Article |
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Drug treatments</subject><subject>Protein Binding</subject><subject>Serotonin - metabolism</subject><subject>Serotonin Receptor Agonists - administration & dosage</subject><subject>Serotonin Receptor Agonists - chemical synthesis</subject><subject>Serotonin Receptor Agonists - pharmacology</subject><subject>Structure-Activity Relationship</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2002</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpNkF1LHTEQhoNU9NT6Eyx7U9GL2JndSc7mUqRfIHphC4VSQjabtLH75SZbOP76Rj1Ur5KZPO9MeBg7QjhDQPn-BpQEXiv6fgLlKQDkinbYCkkSrwjEK7b6j-yz1zHeAiAB0R7bR1RCAYgVu70a_7quuOI_kJ8gj0sTU0hLcm1BfAqTm0Mbhk3Xu_R7051yetH72bjh3vShdbEwsZjG5IZU2LEbh2CLaR7_hMGlfDW_8kN8w3a96aI73J4H7NvHD18vPvPL609fLs4vua0qkbj1vhSlQgGyFaRyBb5tlId6jSDrNXnTeDSVaRW1VBoEQlmbxjpJrlayOmDHT3PzD-4WF5PuQ7Su68zgxiXqNcpsQkAGxRNo5zHG2Xk9zaE380Yj6AfJ-lGyfjCoodSPkjXl3NvtgqXpXfuc2lrNwLstYKI1nZ_NYEN85ipBWNai-gdG5YYr</recordid><startdate>20020325</startdate><enddate>20020325</enddate><creator>HARADA, Hiroshi</creator><creator>YAMAZAKI, Hiroshi</creator><creator>TOYOTOMI, Yoshihito</creator><creator>TATEISHI, Hirotaka</creator><creator>MINE, Yukiko</creator><creator>YOSHIDA, Naoyuki</creator><creator>KATO, Shiro</creator><general>Elsevier</general><scope>IQODW</scope><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>20020325</creationdate><title>Novel N-[1-(1-substituted 4-piperidinylmethyl)-4piperidinyl]benzamides as potent colonic prokinetic agents</title><author>HARADA, Hiroshi ; YAMAZAKI, Hiroshi ; TOYOTOMI, Yoshihito ; TATEISHI, Hirotaka ; MINE, Yukiko ; YOSHIDA, Naoyuki ; KATO, Shiro</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c335t-cff25291506d549ff20fdb9f087106874fabf1a3ad94d42a104168abce64e8963</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2002</creationdate><topic>Animals</topic><topic>Benzamides - administration & dosage</topic><topic>Benzamides - chemical synthesis</topic><topic>Benzamides - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Digestive system</topic><topic>Digestive System - drug effects</topic><topic>Dogs</topic><topic>Gastrointestinal Agents - administration & dosage</topic><topic>Gastrointestinal Agents - chemical synthesis</topic><topic>Gastrointestinal Agents - pharmacology</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding</topic><topic>Serotonin - metabolism</topic><topic>Serotonin Receptor Agonists - administration & dosage</topic><topic>Serotonin Receptor Agonists - chemical synthesis</topic><topic>Serotonin Receptor Agonists - pharmacology</topic><topic>Structure-Activity Relationship</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>HARADA, Hiroshi</creatorcontrib><creatorcontrib>YAMAZAKI, Hiroshi</creatorcontrib><creatorcontrib>TOYOTOMI, Yoshihito</creatorcontrib><creatorcontrib>TATEISHI, Hirotaka</creatorcontrib><creatorcontrib>MINE, Yukiko</creatorcontrib><creatorcontrib>YOSHIDA, Naoyuki</creatorcontrib><creatorcontrib>KATO, Shiro</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>HARADA, Hiroshi</au><au>YAMAZAKI, Hiroshi</au><au>TOYOTOMI, Yoshihito</au><au>TATEISHI, Hirotaka</au><au>MINE, Yukiko</au><au>YOSHIDA, Naoyuki</au><au>KATO, Shiro</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel N-[1-(1-substituted 4-piperidinylmethyl)-4piperidinyl]benzamides as potent colonic prokinetic agents</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2002-03-25</date><risdate>2002</risdate><volume>12</volume><issue>6</issue><spage>967</spage><epage>970</epage><pages>967-970</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A series of novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides was prepared and its compounds were evaluated for their binding to 5-HT(4) receptors and effects on gastrointestinal motility in conscious dogs. 4-Amino-N-[1-[1-(4-aminobutyl)-4-piperidinylmethyl]-4-piperidinyl]-5-chloro-2-methoxybenzamide (15) was found to have a potent binding affinity for 5-HT(4) receptors (IC(50): 6.47nM) and showed excellent colonic prokinetic activity.</abstract><cop>Oxford</cop><pub>Elsevier</pub><pmid>11959005</pmid><doi>10.1016/S0960-894X(02)00060-4</doi><tpages>4</tpages></addata></record> |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2002-03, Vol.12 (6), p.967-970 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Benzamides - administration & dosage Benzamides - chemical synthesis Benzamides - pharmacology Biological and medical sciences Digestive system Digestive System - drug effects Dogs Gastrointestinal Agents - administration & dosage Gastrointestinal Agents - chemical synthesis Gastrointestinal Agents - pharmacology Medical sciences Pharmacology. Drug treatments Protein Binding Serotonin - metabolism Serotonin Receptor Agonists - administration & dosage Serotonin Receptor Agonists - chemical synthesis Serotonin Receptor Agonists - pharmacology Structure-Activity Relationship |
| title | Novel N-[1-(1-substituted 4-piperidinylmethyl)-4piperidinyl]benzamides as potent colonic prokinetic agents |
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