title: Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands.
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.
authors.affiliation: DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Experimental Station, PO Box 80500, 19880, Wilmington, DE 19880, USA. richard.a.hartz@dupontpharm.com
authors.forename: Richard A
authors.initials: RA
authors.lastname: Hartz
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: Kausik K
authors.initials: KK
authors.lastname: Nanda
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Tebben
authors.forename: Larry W
authors.initials: LW
authors.lastname: Fitzgerald
authors.forename: Keith
authors.initials: K
authors.lastname: Miller
mesh_terms: 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
chemical_list: D007093:Imidazoles; D007202:Indicators and Reagents; D008024:Ligands; D011719:Pyrazines; D018019:Receptors, Corticotropin-Releasing Hormone