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  • Title: 5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists.
    Author: Lowe JA, Hageman DL, Drozda SE, McLean S, Bryce DK, Crawford RT, Zorn S, Morrone J, Bordner J.
    Journal: J Med Chem; 1994 Oct 28; 37(22):3789-811. PubMed ID: 7966138.
    Abstract:
    A series of 5-phenyl-3-ureidobenzazepin-2-one cholecystokinin-B (CCK-B) receptor antagonists was synthesized using Beckmann ring expansion of a suitable 4-phenyl-1-tetralone as a key step. Structure-activity relationship studies revealed the importance of the 5-phenyl group for potent and selective CCK-B affinity. Addition of an 8-methyl substituent and resolution provided the potent (CCK-B IC50 = 0.48 nM) CCK-B antagonist 4. The role of the 5-phenyl group as part of a "privileged structure" for high-affinity receptor antagonism is discussed.
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