Abstract
A series of 7,8- and 8,9-fused pyrimidinone, aminopyrimidine 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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Animals
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Azocines / chemical synthesis
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Azocines / chemistry
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Azocines / pharmacology*
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Binding, Competitive / drug effects
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CHO Cells
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Cricetinae
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Cricetulus
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Cyclazocine / analogs & derivatives*
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Cyclazocine / chemical synthesis
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Cyclazocine / chemistry
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Cyclazocine / pharmacology
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Drug Design
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Molecular Conformation
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Narcotic Antagonists*
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Receptors, Opioid / agonists*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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8-carboxamidocyclazocine
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Azocines
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Narcotic Antagonists
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Receptors, Opioid
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Cyclazocine