Electric Literature of C6H5Br2NOOn June 1, 2011, Allcock, Robert W.; Blakli, Haakon; Jiang, Zhong; Johnston, Karen A.; Morgan, Keith M.; Rosair, Georgina M.; Iwase, Kazuhiko; Kohno, Yasushi; Adams, David R. published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast》. The article mentions the following:
Ibudilast [1-(2-isopropylpyrazolo[1,5-a]pyridin-3-yl)-2-methylpropan-1-one] is a nonselective phosphodiesterase inhibitor used clin. to treat asthma. Efforts to selectively develop the PDE3- and PDE4-inhibitory activity of ibudilast led to replacement of the iso-Pr ketone by a pyridazinone heterocycle. Structure-activity relationship exploration in the resulting 6-(pyrazolo[1,5-a]pyridin-3-yl)pyridazin-3(2H)-ones revealed that the pyridazinone lactam functionality is a critical determinant for PDE3-inhibitory activity, with the nitrogen preferably unsubstituted. PDE4 inhibition is strongly promoted by introduction of a hydrophobic substituent at the pyridazinone N(2) center and a methoxy group at C-7′ in the pyrazolopyridine. Migration of the pyridazinone ring connection from the pyrazolopyridine 3′-center to C-4′ strongly enhances PDE4 inhibition. These studies establish a basis for development of potent PDE4-selective and dual PDE3/4-selective inhibitors derived from ibudilast. In addition to this study using 2,3-Dibromo-6-methoxypyridine, there are many other studies that have used 2,3-Dibromo-6-methoxypyridine(cas: 909720-21-4Electric Literature of C6H5Br2NO) was used in this study.
2,3-Dibromo-6-methoxypyridine(cas: 909720-21-4) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Electric Literature of C6H5Br2NO