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Benzotriazonine as a new core structure for the design of CCK-receptor antagonists

✍ Scribed by Achim Escherich; Chantal Escrieut; Daniel Fourmy; Luis Moroder

Publisher: John Wiley and Sons
Year: 1999
Tongue: English
Weight: 68 KB
Volume: 5
Category: Article
ISSN: 1075-2617
DOI: 10.1002/(sici)1099-1387(199903)5:3<155::aid-psc195>3.0.co;2-e

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✦ Synopsis

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.

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