Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands

A novel series of imidazo[1,5- a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored. A novel series of imidazo[1,5- a]...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (3), p.291-294
Hauptverfasser: Hartz, Richard A., Gilligan, Paul J., Nanda, Kausik K., Tebben, Andrew J., Fitzgerald, Larry W., Miller, Keith
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container_end_page 294
container_issue 3
container_start_page 291
container_title Bioorganic & medicinal chemistry letters
container_volume 12
creator Hartz, Richard A.
Gilligan, Paul J.
Nanda, Kausik K.
Tebben, Andrew J.
Fitzgerald, Larry W.
Miller, Keith
description A novel series of imidazo[1,5- a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands. SAR studies focused primarily on dialkylamino side chain optimization. SAR of the aryl and small alkyl substituents was also explored. A novel series of imidazo[1,5- a]pyrazines was synthesized and evaluated as corticotropin releasing hormone (CRH) receptor ligands.
doi_str_mv 10.1016/S0960-894X(01)00741-7
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source MEDLINE; Elsevier ScienceDirect Journals
subjects Alkylation
Animals
Binding, Competitive - drug effects
Biological and medical sciences
Imidazoles - chemical synthesis
Imidazoles - pharmacology
In Vitro Techniques
Indicators and Reagents
Ligands
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Prefrontal Cortex - metabolism
Pyrazines - chemical synthesis
Pyrazines - pharmacology
Rats
Receptors, Corticotropin-Releasing Hormone - antagonists & inhibitors
Structure-Activity Relationship
title Synthesis and evaluation of imidazo[1,5- a]pyrazines as corticotropin releasing hormone receptor ligands
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