Da Settimo, Federico published the artcile[1,2,4]Triazino[4,3-a]benzimidazole Acetic Acid Derivatives: A New Class of Selective Aldose Reductase Inhibitors, SDS of cas: 76283-09-5, the publication is Journal of Medicinal Chemistry (2001), 44(25), 4359-4369, database is CAplus and MEDLINE.
Acetic acid derivatives of [1,2,4]triazino[4,3-a]benzimidazole (TBI) were synthesized and tested in vitro and in vivo as a novel class of aldose reductase (ALR2) inhibitors. (10-Benzyl[1,2,4]triazino[4,3-a]benzimidazole-3,4(10H)-dion-2-yl)acetic acid (I), displayed the highest inhibitory activity (IC50 = 0.36 μM) and effective in preventing cataract development in severely galactosemic rats when administered as an eyedrop solution All the compounds investigated were selective for ALR2, since none of them inhibited appreciably aldehyde reductase, sorbitol dehydrogenase, or glutathione reductase. The activity of I was lowered by inserting various substituents on the pendant Ph ring, by shifting the acetic acid moiety from the 2 to the 3 position of the TBI nucleus, or by cleaving the TBI system to yield benzimidazolylidenehydrazines as open-chain analogs. A three-dimensional model of human ALR2 was built, taking into account the conformational changes induced by the binding of inhibitors such as zopolrestat, to simulate the docking of I into the enzyme active site. The theor. binding mode of I was fully consistent with the structure-activity relationships in the TBI series and will guide the design of novel ALR2 inhibitors.
Journal of Medicinal Chemistry published new progress about 76283-09-5. 76283-09-5 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Benzyl bromide,Benzene, name is 4-Bromo-1-(bromomethyl)-2-fluorobenzene, and the molecular formula is C7H5Br2F, SDS of cas: 76283-09-5.
Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary