title: Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.
abstract: A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series.
authors.affiliation: Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI 48105, USA.
authors.forename: D J
authors.initials: DJ
authors.lastname: Wustrow
authors.forename: T
authors.initials: T
authors.lastname: Capiris
authors.forename: R
authors.initials: R
authors.lastname: Rubin
authors.forename: J A
authors.initials: JA
authors.lastname: Knobelsdorf
authors.forename: H
authors.initials: H
authors.lastname: Akunne
authors.forename: M D
authors.initials: MD
authors.lastname: Davis
authors.forename: R
authors.initials: R
authors.lastname: MacKenzie
authors.forename: T A
authors.initials: TA
authors.lastname: Pugsley
authors.forename: K T
authors.initials: KT
authors.lastname: Zoski
authors.forename: T G
authors.initials: TG
authors.lastname: Heffner
authors.forename: L D
authors.initials: LD
authors.lastname: Wise
mesh_terms: D003346:Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D018360:Crystallography, X-Ray; D015195:Drug Design; D006801:Humans; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
chemical_list: D011720:Pyrazoles; D011743:Pyrimidines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1; D003346:Corticotropin-Releasing Hormone