Abstract
A series of 2-substituted sulfamoyl arylacetamides of general structure 2 were prepared as potent kappa opioid receptor agonists and the affinities of these compounds for opioid and chimeric receptors were compared with those of dynorphin A. Compounds 2e and 2i were identified as non-peptide small molecules that bound to chimeras 3 and 4 with high affinities similar to dynorphin A, resulting in K(i) values of 1.5 and 1.2 nM and 1.3 and 2.2 nM, respectively.
MeSH terms
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Acetamides / chemical synthesis
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Acetamides / chemistry
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Acetamides / pharmacology*
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Binding Sites / drug effects
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Dose-Response Relationship, Drug
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Drug Evaluation, Preclinical
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Dynorphins / chemistry
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Dynorphins / pharmacology*
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Molecular Structure
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Molecular Weight
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Receptors, Opioid, kappa / agonists*
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Receptors, Opioid, kappa / chemistry
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Receptors, Opioid, kappa / genetics
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Recombinant Fusion Proteins / agonists*
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Recombinant Fusion Proteins / chemistry
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Recombinant Fusion Proteins / genetics
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Small Molecule Libraries
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Acetamides
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Receptors, Opioid, kappa
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Recombinant Fusion Proteins
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Small Molecule Libraries
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Dynorphins