Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 6. Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine

A series of 7,8- and 8,9-fused pyrimidinone, aminopyridine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in opioid receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carb...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-03, Vol.16 (10), p.5653-5664
Main Authors: Wentland, Mark P., Sun, Xufeng, Cohen, Dana J., Bidlack, Jean M.
Format: Article
Language:English
Online Access:Get full text
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Summary:A series of 7,8- and 8,9-fused pyrimidinone, aminopyridine and pyridone derivatives of 8-carboxamidocyclazocine (8-CAC) have been prepared and evaluated in opioid receptor binding assays. Targets were designed to corroborate a pharmacophore hypothesis regarding the bioactive conformation of the carboxamide of 8-CAC. In addition to the results from this study strongly supporting this pharmacophore hypothesis, a number of novel compounds with high affinity to opioid receptors have been identified.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2008.03.066