In 2019,Journal of Enzyme Inhibition and Medicinal Chemistry included an article by Elie, Jonathan; Vercouillie, Johnny; Arlicot, Nicolas; Lemaire, Lucas; Bidault, Rudy; Bodard, Sylvie; Hosselet, Christel; Deloye, Jean-Bernard; Chalon, Sylvie; Emond, Patrick; Guilloteau, Denis; Buron, Frederic; Routier, Sylvain. Related Products of 128071-75-0. The article was titled 《Design of selective COX-2 inhibitors in the (aza)indazole series. Chemistry, in vitro studies, radiochemistry and evaluations in rats of a [18F] PET tracer》. The information in the text is summarized as follows:
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. The experimental part of the paper was very detailed, including the reaction process of 2-Bromonicotinaldehyde(cas: 128071-75-0Related Products of 128071-75-0)
2-Bromonicotinaldehyde(cas: 128071-75-0) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.Related Products of 128071-75-0