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Eur J Med Chem. 2010 Mar;45(3):909-14. doi: 10.1016/j.ejmech.2009.11.031. Epub 2009 Dec 4.

Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors.

Author information

1
Sri Vasavi Institute of Pharmaceutical Sciences, Pedatadepalli, Tadepalligudem, West Godavari District 534101, Andhra Pradesh, India. psahoo.phar@gmail.com

Abstract

The acetic acid derivatives of [1,2,4]triazino[4,3-a]benzimidazole (TBI) were synthesized and tested in vitro and in vivo as selective aldose reductase (ALR2) inhibitors. Compound PS11 showed highest inhibitory activity (IC(50)) 0.32 microM and was found to be 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.

PMID:
19962793
DOI:
10.1016/j.ejmech.2009.11.031
[Indexed for MEDLINE]

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