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Benzotriazonine as a new core structure for the design of CCK‐receptor antagonists
Author(s) -
Escherich Achim,
Escrieut Chantal,
Fourmy Daniel,
Moroder Luis
Publication year - 1999
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/(sici)1099-1387(199903)5:3<155::aid-psc195>3.0.co;2-e
Subject(s) - receptor , chemistry , peptide , gastrin , stereochemistry , selectivity , cholecystokinin receptor , peptide hormone , antagonist , pharmacology , combinatorial chemistry , biochemistry , biology , secretion , catalysis
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‐1 H ‐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.