title: Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
abstract: A series of purin-8-ones was prepared and discovered to have excellent binding affinity to the CRH-R1 receptor. Structure-activity studies focused on amine side-chain optimization, urea substitution and pyridyl isostere incorporation. Thus, the highly potent purin-8-ones show promise as a new class of potential anxiolytics and/or antidepressants.
authors.affiliation: DuPont Pharmaceuticals Company, Chemical and Physical Sciences, Wilmington, DE 19880-0500, USA.
authors.forename: J P
authors.initials: JP
authors.lastname: Beck
authors.forename: A G
authors.initials: AG
authors.lastname: Arvanitis
authors.forename: M A
authors.initials: MA
authors.lastname: Curry
authors.forename: J T
authors.initials: JT
authors.lastname: Rescinito
authors.forename: L W
authors.initials: LW
authors.lastname: Fitzgerald
authors.forename: P J
authors.initials: PJ
authors.lastname: Gilligan
authors.forename: R
authors.initials: R
authors.lastname: Zaczek
authors.forename: G L
authors.initials: GL
authors.lastname: Trainor
mesh_terms: D014151:Anti-Anxiety Agents / Q000737:chemistry / Q000494:pharmacology; D000928:Antidepressive Agents / Q000737:chemistry / Q000494:pharmacology; D011688:Purinones / Q000737:chemistry / Q000494:pharmacology*; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
chemical_list: D014151:Anti-Anxiety Agents; D000928:Antidepressive Agents; D011688:Purinones; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1