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
Format:	Artikel
Sprache:	eng
Schlagworte:	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
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00741-7