So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Dias, Maria C. F.; Gularte, Thiago Q.; Teixeira, Robson R.; Santos, Jorge A. N.; Pilau, Eduardo J.; Mendes, Tiago A. O.; Demuner, Antonio J.; dos Santos, Marcelo H. researched the compound: 1-(Bromomethyl)-4-iodobenzene( cas:16004-15-2 ).Application of 16004-15-2.They published the article 《Synthesis of 1,2,3-triazole derivatives of 4,4′-dihydroxybenzophenone and evaluation of their elastase inhibitory activity》 about this compound( cas:16004-15-2 ) in Journal of the Brazilian Chemical Society. Keywords: benzophenone bis aryl triazolylmethoxy preparation elastase inhibitor docking. We’ll tell you more about this compound (cas:16004-15-2).
The synthesis of a series of novel triazole derivatives I (R = 4-iodophenyl, 2-methylphenyl, 2,6-dichlorophenyl, etc.) from 4,4′-dihydroxybenzophenone along with their elastase inhibitory activity has been described. The 1,2,3-triazoles I were obtained via the copper(I)-catalyzed azide-alkyne cycloaddition reaction (CuAAC), also known as click reaction, between bis(4-(prop-2-yn-1-yloxy))benzophenone and several benzyl azides RCH2N3. It was found that five derivatives exhibited significant inhibitory effects, presenting half maximal inhibitory concentration (IC50) values in the range of 16.6 to 72.1 μM. The most active compound, namely I (R = 4-iodophenyl) (IC50 = 16.6 ± 1.9 μM), was found to bind to elastase with the inhibition constant (Ki) of 11.12 μM, thereby illustrating competitive inhibitory behavior. Further, docking investigations provided insights on the possible binding mode of the most active compound with the elastase.
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Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics