title: 5-arylamino-1,2,4-triazin-6(1H)-one CRF1 receptor antagonists.
abstract: A series of 5-arylamino-1,2,4-triazin-6(1H)-ones was synthesized and evaluated as antagonists at the corticotropin releasing factor receptor. Formation of CYP-mediated oxidative reactive metabolites previously observed in a related N(3)-phenylpyrazinone structure was minimized by incorporation of the additional ring nitrogen found in the triazinones.
authors.affiliation: Neuroscience Discovery Chemistry, Bristol-Myers Squibb Research and Development, Wallingford, CT 06492, USA. william.schmitz@bms.com
authors.forename: William D
authors.initials: WD
authors.lastname: Schmitz
authors.forename: Allison B
authors.initials: AB
authors.lastname: Brenner
authors.forename: Joanne J
authors.initials: JJ
authors.lastname: Bronson
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Ditta
authors.forename: Corrine R
authors.initials: CR
authors.lastname: Griffin
authors.forename: Yu-Wen
authors.initials: YW
authors.lastname: Li
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Lodge
authors.forename: Thaddeus F
authors.initials: TF
authors.lastname: Molski
authors.forename: Richard E
authors.initials: RE
authors.lastname: Olson
authors.forename: Xiaoliang
authors.initials: X
authors.lastname: Zhuo
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
mesh_terms: D000818:Animals; D006801:Humans; D020128:Inhibitory Concentration 50; D010084:Oxidation-Reduction; D011719:Pyrazines; D051381:Rats; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000099052:CRF Receptor, Type 1
chemical_list: D011719:Pyrazines; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D000099052:CRF Receptor, Type 1