Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model was written by La Motta, Concettina;Sartini, Stefania;Salerno, Silvia;Simorini, Francesca;Taliani, Sabrina;Marini, Anna Maria;Da Settimo, Federico;Marinelli, Luciana;Limongelli, Vittorio;Novellino, Ettore. And the article was included in Journal of Medicinal Chemistry in 2008.Reference of 422560-40-5 The following contents are mentioned in the article:
A number of 1,2,4-oxadiazol-5-ylacetic acids and oxazol-4-ylacetic acids were synthesized and tested for their ability to inhibit aldose reductase (ALR2). Several oxadiazole derivatives proved to be the most active compounds, exhibiting inhibitory levels in the submicromolar range. In this series, the Ph group turned out to be the preferred substitution pattern, as its lengthening to a benzyl moiety determined a general reduction of the inhibitory potency. The lead compound, 2-[3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl]acetic acid, showed an excellent in vivo activity, proving to prevent cataract development in severely galactosemic rats when administered as an eye-drop solution in the precorneal region of the animals. Computational studies on the ALR2 inhibitors were performed to rationalize the structure-activity relationships observed and to provide the basis for further structure-guided design of novel ALR2 inhibitors. This study involved multiple reactions and reactants, such as 2-(4-Bromophenyl)-N-hydroxyacetimidamide (cas: 422560-40-5Reference of 422560-40-5).
2-(4-Bromophenyl)-N-hydroxyacetimidamide (cas: 422560-40-5) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Reference of 422560-40-5
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary