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

Richard A Hartz; Paul J Gilligan; Kausik K Nanda; Andrew J Tebben; Larry W Fitzgerald; Keith Miller

doi:10.1016/s0960-894x(01)00741-7

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

Bioorg Med Chem Lett. 2002 Feb 11;12(3):291-4. doi: 10.1016/s0960-894x(01)00741-7.

Authors

Richard A Hartz¹, Paul J Gilligan, Kausik K Nanda, Andrew J Tebben, Larry W Fitzgerald, Keith Miller

Affiliation

¹ DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Experimental Station, PO Box 80500, 19880, Wilmington, DE 19880, USA. richard.a.hartz@dupontpharm.com

PMID: 11814780
DOI: 10.1016/s0960-894x(01)00741-7

Abstract

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.

MeSH terms

Alkylation
Animals
Binding, Competitive / drug effects
Imidazoles / chemical synthesis*
Imidazoles / pharmacology*
In Vitro Techniques
Indicators and Reagents
Ligands
Prefrontal Cortex / metabolism
Pyrazines / chemical synthesis*
Pyrazines / pharmacology*
Rats
Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Imidazoles
Indicators and Reagents
Ligands
Pyrazines
Receptors, Corticotropin-Releasing Hormone