Abstract
A series of N-8 substituted analogs based upon the spiropiperidine core of the original lead compound 1 was synthesized. This lead has been elaborated to compounds to give compounds 2 and 3 (R=H) that exhibited high NOP binding affinity as well as selectivity against other known opioid receptors. These two series have been further functionalized at the amido nitrogen. The synthesis and structure-activity relationship (SAR) of these and related compounds are discussed.
MeSH terms
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Animals
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Binding Sites
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Capsaicin / pharmacology
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Combinatorial Chemistry Techniques
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Cough / chemically induced
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Disease Models, Animal
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Drug Design
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Guinea Pigs
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Molecular Structure
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Nociceptin Receptor
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Piperidines / chemical synthesis*
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Piperidines / chemistry
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Piperidines / pharmacology*
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Receptors, Opioid / drug effects*
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Receptors, Opioid / metabolism
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Spiro Compounds / chemical synthesis*
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacology*
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Structure-Activity Relationship
Substances
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Piperidines
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Receptors, Opioid
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Spiro Compounds
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Capsaicin
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Nociceptin Receptor