title: Potential CRF1R PET imaging agents: N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines.
abstract: A series of N-fluoroalkyl-8-(6-methoxy-2-methylpyridin-3-yl)-2,7-dimethyl-N-alkylpyrazolo[1,5-a][1,3,5]triazin-4-amines were prepared and evaluated as potential CRF(1)R PET imaging agents. Optimization of their CRF(1)R binding potencies and octanol-phosphate buffer phase distribution coefficients resulted in discovery of analog 7e (IC(50)=6.5 nM, logD=3.5).
authors.affiliation: Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. dmitry.zuev@bms.com
authors.forename: Dmitry
authors.initials: D
authors.lastname: Zuev
authors.forename: Ronald J
authors.initials: RJ
authors.lastname: Mattson
authors.forename: Hong
authors.initials: H
authors.lastname: Huang
authors.forename: Gail K
authors.initials: GK
authors.lastname: Mattson
authors.forename: Larisa
authors.initials: L
authors.lastname: Zueva
authors.forename: Julia M
authors.initials: JM
authors.lastname: Nielsen
authors.forename: Edward S
authors.initials: ES
authors.lastname: Kozlowski
authors.forename: Xiaohua Stella
authors.initials: XS
authors.lastname: Huang
authors.forename: Dedong
authors.initials: D
authors.lastname: Wu
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
authors.forename: Nicholas J
authors.initials: NJ
authors.lastname: Lodge
authors.forename: Joanne J
authors.initials: JJ
authors.lastname: Bronson
authors.forename: John E
authors.initials: JE
authors.lastname: Macor
mesh_terms: D000588:Amines / Q000138:chemical synthesis / Q000737:chemistry*; D018360:Crystallography, X-Ray; D008968:Molecular Conformation; D049268:Positron-Emission Tomography; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry*; D018019:Receptors, Corticotropin-Releasing Hormone / Q000737:chemistry* / Q000378:metabolism; D014227:Triazines / Q000138:chemical synthesis / Q000737:chemistry*; D000099052:CRF Receptor, Type 1
chemical_list: D000588:Amines; D011720:Pyrazoles; D018019:Receptors, Corticotropin-Releasing Hormone; D014227:Triazines; D000099052:CRF Receptor, Type 1