Hu, Essa published the artcileDiscovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors, HPLC of Formula: 1366482-32-7, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(6), 2262-2265, database is CAplus and MEDLINE.
Aminopyridinyl-substituted dimethoxycinnolines such as piperidinylpyridinyl dimethoxycinnolines I (R = H, Me, Cl, F2CH, cyclopropyl; R1 = HO, HOCMe2; R2 = H, Me, cyclopropyl, 2-pyridinyl) were prepared as selective inhibitors of phosphodiesterase 10A (PDE10A) for potential use in the treatment of schizophrenia. Bromodimethoxycinnoline II was prepared in two steps from 2-amino-4,5-dimethoxyacetophenone; Suzuki coupling of II with fluoropyridinyl boronic acids followed by aryl substitution reactions with amines and nitrogen heterocycles yielded aminopyridinyl-substituted dimethoxycinnolines. I (R = H, Me, Cl, F2CH, cyclopropyl; R1 = HO, HOCMe2; R2 = H, Me, cyclopropyl, 2-pyridinyl) inhibited PDE10A with IC50 values of 1.3-13.2 nM and were selective for PDE10A over phosphodiesterases 1-9 and 11 (particularly PDE3) by greater than 350-fold. I (R = H, Me, Cl, F2CH, cyclopropyl; R1 = HO, HOCMe2; R2 = H, Me, cyclopropyl, 2-pyridinyl), in which the piperidinyl moiety was hydroxy- or hydroxyalkyl-substituted, showed reduced clearance in rats [0.15-2.15 L/(h × kg)] relative to methoxyethyl- and methoxyazetidinyl-substituted pyridinyl cinnolines. I (R = Me; R1 = HO; R2 = 2-pyridinyl) suppressed the conditioned avoidance response in rats (a model of schizophrenia) at a dosage of 5.6 mg/kg. The structure of I (R = Me; R1 = HOCMe2; R2 = H) bound to the catalytic domain of human PDE10A was determined by X-ray crystallog.
Bioorganic & Medicinal Chemistry Letters published new progress about 1366482-32-7. 1366482-32-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Fluoride,Chloride,Boronic acid and ester,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (5-Chloro-6-fluoropyridin-3-yl)boronic acid, and the molecular formula is C5H4BClFNO2, HPLC of Formula: 1366482-32-7.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem