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
Hauptverfasser: Escherich, Achim, Escrieut, Chantal, Fourmy, Daniel, Moroder, Luis
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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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source MEDLINE; Wiley Journals
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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