| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2013: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Outline of Final Research Achievements |
Aldose reductase (ALR2) is associated with the onset of diabetic complications, and therefore ALR2 inhibitors has attracted attentions of medicinal chemists. Despite numerous devotions of the researchers, only one drug, epalrestat, has been launched on the market, and accordingly the development of new candidates for ALR2 inhibitors is still desired. The present work revealed that botryllazine B analogues possessing diverse substituted phenylcarbonyl groups on the 2-position and various fused bicyclic aromatic systems on the 6-position, pterin-7-carboxamides, and (Z)-4-arylmethylidene-1H-imidazol-5(4H)-ones (GFP chromophore model compounds) are highly potent ALR2 inhibitors. Docking simulations of these compounds also revealed that each of them exhibited specific interaction with ALR2. In conclusion, the compounds synthesized in this study have proved to be potential drugs for diabetic complications.
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