Elie, Jonathan published the artcileDesign of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer, Quality Control of 612845-44-0, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2019), 34(1), 1-7, database is CAplus and MEDLINE.
A series of novel derivatives exhibiting high affinity and selectivity towards the COX-2 enzyme in the (aza) indazole series was developed. A short synthetic route involving a bromination/arylation sequence under microwave irradiation and direct C-H activation were established in the indazole and azaindazole series resp. In vitro assays were conducted and structural modifications were carried out on these scaffolds to furnish compound which exhibited effective COX-2 inhibitory activity, with IC50 values of 0.409 μM and an excellent selectivity vs. COX-1. Radiolabeling of this most potent derivative [18F] was achieved after boron ester release and the tracer was evaluated in vivo in a rat model of neuroinflammation. All chem., radiochem. and biol. exptl. data are discussed.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 612845-44-0. 612845-44-0 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Ether,Boronic Acids,Boronic acid and ester, name is (6-Ethoxypyridin-3-yl)boronic acid, and the molecular formula is C7H10BNO3, Quality Control of 612845-44-0.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem