5,7-Diphenyl-3-ureidohexahydroazepin-2-ones as Cholecystokinin-B receptor ligands |
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| Authors: | John A Lowe III Weimin Qian Pamela J Scott Stafford McLean Dianne K Bryce Rosemary T Crawford Jon Bordner |
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| Institution: | Central Research Division, Pfizer Inc Eastern Point Road, Groton, CT 06340 U.S.A. |
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| Abstract: | A series of 5,7-diphenyl-3-ureidohexahydroazepin-2-one cholecystokinin-B (CCK-B) receptor antagonists was synthesized using Beckmann ring expansion of a suitable 2,4-diphenylcyclohexanone as a key step. SAR studies revealed the importance of the 5-aryl group for high and selective CCK-B receptor affinity, as illustrated in compound (−)-10i (CCK-B IC50 = 6.8 nM). |
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