Abstract
Low nanomolar corticotropin releasing factor type-1 (CRF(1)) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K(i)=11+/-1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine.
MeSH terms
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Binding, Competitive / drug effects
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CRF Receptor, Type 1
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Catalysis
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Copper / chemistry
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Drug Evaluation, Preclinical
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Humans
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Indans / chemistry*
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Molecular Structure
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Pyrazines / chemistry*
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Pyrazines / metabolism
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Pyrazines / pharmacology*
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Pyridones / chemistry
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Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
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Receptors, Corticotropin-Releasing Hormone / metabolism
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Structure-Activity Relationship
Substances
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Indans
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Pyrazines
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Pyridones
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Receptors, Corticotropin-Releasing Hormone
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CRF Receptor, Type 1
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Copper