Benzotriazonine as a new core structure for the design of CCK-receptor antagonists
The search for heterocyclic scaffolds for the design of non‐peptidic and highly selective agonists or antagonists of peptide hormone receptors led to 4‐N‐benzyl‐2,3,4,5,6,7‐hexahydro‐1H‐1,4,7‐benzotriazonin‐2,6‐dione with a 9‐membered core structure as a new low mass lead compound that exhibits subm...
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Veröffentlicht in: | Journal of peptide science 1999-03, Vol.5 (3), p.155-158 |
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container_title | Journal of peptide science |
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creator | Escherich, Achim Escrieut, Chantal Fourmy, Daniel Moroder, Luis |
description | The search for heterocyclic scaffolds for the design of non‐peptidic and highly selective agonists or antagonists of peptide hormone receptors led to 4‐N‐benzyl‐2,3,4,5,6,7‐hexahydro‐1H‐1,4,7‐benzotriazonin‐2,6‐dione with a 9‐membered core structure as a new low mass lead compound that exhibits submicromolar antagonistic activity at the CCK‐A receptor with a 54‐fold selectivity over the CCK‐B/gastrin receptor. Copyright © 1999 European Peptide Society and John Wiley & Sons, Ltd. |
doi_str_mv | 10.1002/(SICI)1099-1387(199903)5:3<155::AID-PSC195>3.0.CO;2-E |
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Peptide Sci</addtitle><description>The search for heterocyclic scaffolds for the design of non‐peptidic and highly selective agonists or antagonists of peptide hormone receptors led to 4‐N‐benzyl‐2,3,4,5,6,7‐hexahydro‐1H‐1,4,7‐benzotriazonin‐2,6‐dione with a 9‐membered core structure as a new low mass lead compound that exhibits submicromolar antagonistic activity at the CCK‐A receptor with a 54‐fold selectivity over the CCK‐B/gastrin receptor. Copyright © 1999 European Peptide Society and John Wiley & Sons, Ltd.</description><subject>Animals</subject><subject>benzotriazonine</subject><subject>CCK</subject><subject>CCK-receptor antagonists</subject><subject>CHO Cells - metabolism</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Cricetinae</subject><subject>Crystallization</subject><subject>Drug Design</subject><subject>gastrin</subject><subject>peptide hormone</subject><subject>Receptor, Cholecystokinin A</subject><subject>Receptor, Cholecystokinin B</subject><subject>Receptors, Cholecystokinin - antagonists & inhibitors</subject><subject>Receptors, Cholecystokinin - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Triazines - chemical synthesis</subject><subject>Triazines - chemistry</subject><subject>Triazines - metabolism</subject><issn>1075-2617</issn><issn>1099-1387</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkdtu1DAQQCMEohf4BZQn1D5k8SW24-UilbAtC6VbUdA-jhx3XAK7ydZOVNqvx1FWFRIInjyaGZ8ZzUmS15RMKCHsxcHFvJwfUqJ1RnmhDqjWmvBDMeWvqBDT6dH8XXZ-UVIt3vAJmZSLlyybPUh27388HGIlMiap2kn2QvhOSKwJ-TjZoYQzLoTeTT6_xeau7Xxt7tqmbjA1ITVpgzepbT2mofO97foYudan3TdMLzHUV03aurQsP2YeLW66WDJNZ64iIXThSfLImVXAp9t3P_l6PPtSvs9OFyfz8ug0sznP416VK5BwYfOCGVEYGXdzyklDlSYyZzlDhyK3lXay0LbgBC2RlbSoLFa64PvJ85G78e11j6GDdR0srlamwbYPILXKudb0v42MUqEoG4jbTa1vQ_DoYOPrtfG3QAkMVgAGKzDcGIYbw2gFBHCIVgCiFRitxAyBcgEMZpH7bLtAX63x8jfqqCE2LMeGm3qFt39M_ffQv87cZiI5G8nRDP68Jxv_A6TiSsDy7AQ-FGe8OF9-gmP-C6vXtto</recordid><startdate>199903</startdate><enddate>199903</enddate><creator>Escherich, Achim</creator><creator>Escrieut, Chantal</creator><creator>Fourmy, Daniel</creator><creator>Moroder, Luis</creator><general>John Wiley & Sons, Ltd</general><scope>BSCLL</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>199903</creationdate><title>Benzotriazonine as a new core structure for the design of CCK-receptor antagonists</title><author>Escherich, Achim ; Escrieut, Chantal ; Fourmy, Daniel ; Moroder, Luis</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4345-2bf8e035c482a58a6995f7f6a179064242efe54cb9f689c830ec06b6ce7ceb983</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Animals</topic><topic>benzotriazonine</topic><topic>CCK</topic><topic>CCK-receptor antagonists</topic><topic>CHO Cells - metabolism</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Cricetinae</topic><topic>Crystallization</topic><topic>Drug Design</topic><topic>gastrin</topic><topic>peptide hormone</topic><topic>Receptor, Cholecystokinin A</topic><topic>Receptor, Cholecystokinin B</topic><topic>Receptors, Cholecystokinin - antagonists & inhibitors</topic><topic>Receptors, Cholecystokinin - metabolism</topic><topic>Structure-Activity Relationship</topic><topic>Triazines - chemical synthesis</topic><topic>Triazines - chemistry</topic><topic>Triazines - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Escherich, Achim</creatorcontrib><creatorcontrib>Escrieut, Chantal</creatorcontrib><creatorcontrib>Fourmy, Daniel</creatorcontrib><creatorcontrib>Moroder, Luis</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of peptide science</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Escherich, Achim</au><au>Escrieut, Chantal</au><au>Fourmy, Daniel</au><au>Moroder, Luis</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Benzotriazonine as a new core structure for the design of CCK-receptor antagonists</atitle><jtitle>Journal of peptide science</jtitle><addtitle>J. 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language | eng |
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subjects | Animals benzotriazonine CCK CCK-receptor antagonists CHO Cells - metabolism Chromatography, High Pressure Liquid Cricetinae Crystallization Drug Design gastrin peptide hormone Receptor, Cholecystokinin A Receptor, Cholecystokinin B Receptors, Cholecystokinin - antagonists & inhibitors Receptors, Cholecystokinin - metabolism Structure-Activity Relationship Triazines - chemical synthesis Triazines - chemistry Triazines - metabolism |
title | Benzotriazonine as a new core structure for the design of CCK-receptor antagonists |
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