Abstract
The combination of a 3,5-bis(trifluoromethyl)phenyl needle with the spiropyrrolo-pyrrole motive as a privileged GPCR scaffold was the basis for designing a focused combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase method is described and binding affinities of representative compounds are presented.
MeSH terms
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Combinatorial Chemistry Techniques
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GTP-Binding Proteins / metabolism
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Indicators and Reagents
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Ligands
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Pyrroles / chemical synthesis*
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Pyrroles / pharmacology*
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Receptors, Neurokinin-1 / drug effects
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Receptors, Neurokinin-1 / metabolism*
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Receptors, Neurokinin-2 / drug effects
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Receptors, Neurokinin-2 / metabolism*
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Receptors, Neurokinin-3 / drug effects
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Receptors, Neurokinin-3 / metabolism*
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Structure-Activity Relationship
Substances
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Indicators and Reagents
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Ligands
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Pyrroles
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Receptors, Neurokinin-1
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Receptors, Neurokinin-2
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Receptors, Neurokinin-3
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GTP-Binding Proteins