Abstract
A novel strategy for the synthesis of cholecystokinin-2 receptor ligands was developed. The route employs a solution-phase synthesis of a series of anthranilic sulfonamides followed by a resin capture purification strategy to produce multi-milligram quantities of compounds for bioassay. The synthesis was used to produce >100 compounds containing various functional groups, highlighting the general applicability of this strategy and to address specific metabolism issues in our CCK-2 program.
MeSH terms
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Animals
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Cholecystokinin / metabolism*
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Combinatorial Chemistry Techniques*
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Drug Design
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Humans
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Ligands
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Microsomes, Liver / drug effects
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Molecular Structure
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Rats
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Receptor, Cholecystokinin B / metabolism*
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
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ortho-Aminobenzoates / chemical synthesis*
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ortho-Aminobenzoates / chemistry
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ortho-Aminobenzoates / pharmacology*
Substances
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Ligands
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Receptor, Cholecystokinin B
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Sulfonamides
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ortho-Aminobenzoates
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Cholecystokinin