Discovery of 3-[(4, 5, 7-trifluorobenzothiazol-2-yl) methyl] indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase …

…, JH Jones, DR Sawicki, J Sredy, JL Jacot…

Index: Van Zandt, Michael C.; Jones, Michael L.; Gunn, David E.; Geraci, Leo S.; Jones, J. Howard; Sawicki, Diane R.; Sredy, Janet; Jacot, Jorge L.; DiCioccio, A. Thomas; Petrova, Tatiana; Mitschler, Andre; Podjarny, Alberto D. Journal of Medicinal Chemistry, 2005 , vol. 48, # 9 p. 3141 - 3152

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Citation Number: 150

Abstract

Recent efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective 3-[(benzothiazol-2-yl) methyl] indole-N-alkanoic acid aldose reductase inhibitors. The lead candidate, 3-[(4, 5, 7- trifluorobenzothiazol-2-yl) methyl] indole-N-acetic acid (lidorestat, 9) inhibits aldose reductase with an IC50 of 5 nM, while being 5400 times less active against aldehyde ...