7229-53-0Relevant academic research and scientific papers
Inhibition of copper-mediated aggregation of human γD-crystallin by Schiff bases
Chauhan, Priyanka,Muralidharan, Sai Brinda,Velappan, Anand Babu,Datta, Dhrubajyoti,Pratihar, Sanjay,Debnath, Joy,Ghosh, Kalyan Sundar
, p. 505 - 517 (2017/06/05)
Abstract: Protein aggregation, due to the imbalance in the concentration of Cu2+ and Zn2+ ions is found to be allied with various physiological disorders. Copper is known to promote the oxidative damage of β/γ-crystallins in aged eye lens and causes their aggregation leading to cataract. Therefore, synthesis of a small-molecule ‘chelator’ for Cu2+ with complementary antioxidant effect will find potential applications against aggregation of β/γ-crystallins. In this paper, we have reported the synthesis of different Schiff bases and studied their Cu2+ complexation ability (using UV–Vis, FT-IR and ESI-MS) and antioxidant activity. Further based on their copper complexation efficiency, Schiff bases were used to inhibit Cu2+-mediated aggregation of recombinant human γD-crystallin (HGD) and β/γ-crystallins (isolated from cataractous human eye lens). Among these synthesized molecules, compound 8 at a concentration of 100 μM had shown ~95% inhibition of copper (100?μM)-induced aggregation. Compound 8 also showed a positive cooperative effect at a concentration of 5–15 μM on the inhibitory activity of human αA-crystallin (HAA) during Cu2+-induced aggregation of HGD. It eventually inhibited the aggregation process by additional ~20%. However, ~50% inhibition of copper-mediated aggregation of β/γ-crystallins (isolated from cataractous human eye lens) was recorded by compound 8 (100 μM). Although the reductive aminated products of the imines showed better antioxidant activity due to their lower copper complexing ability, they were found to be non-effective against Cu2+-mediated aggregation of HGD. Graphical Abstract: [Figure not available: see fulltext.]
Benzimidazole derivatives and process for the production thereof
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, (2008/06/13)
Benzimidazoles of the formula STR1 wherein R1 is o-hydroxyphenyl, a p-chlorophenyl, or p-fluorophenyl, and R2 is an alkyl of 2-4 carbon atoms, and physiologically acceptable acid addition salts thereof possess topical anti-inflammato
