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.
Hartz
Richard A
RA
DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Experimental Station, PO Box 80500, 19880, Wilmington, DE 19880, USA. richard.a.hartz@dupontpharm.com
Gilligan
Paul J
PJ
Nanda
Kausik K
KK
Tebben
Andrew J
AJ
Fitzgerald
Larry W
LW
Miller
Keith
K
D000478:Alkylation; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008024:Ligands; D017397:Prefrontal Cortex / Q000378:metabolism; D011719:Pyrazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D007093:Imidazoles; D007202:Indicators and Reagents; D008024:Ligands; D011719:Pyrazines; D018019:Receptors, Corticotropin-Releasing Hormone