Federico Da Settimo,*, Giampaolo Primofiore, Antonio Da Settimo, Concettina La Motta, Sabrina Taliani

F Simorini, E Novellino, G Greco, A Lavecchia…

Index: Da Settimo; Boldrini; Primofiore; La Motta; Taliani; Simorini; Novellino; Greco; Lavecchia Journal of Medicinal Chemistry, 2001 , vol. 44, # 25 p. 4359 - 4369

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Abstract

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. Compound 3,(10-benzyl [1, 2, 4] triazino [4, 3-a] benzimidazol-3, 4 (10H)-dion-2-yl) acetic acid, displayed the highest inhibitory activity (IC50) 0.36 µM) and was found to be effective in preventing cataract development in severely galactosemic rats when administered as an ...