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Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.

Abstract : Efforts to identify treatments for chronic diabetic complications have resulted in the discovery of a novel series of highly potent and selective [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid aldose reductase inhibitors. The lead candidate, [6-methyl-3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acid example 16, inhibits aldose reductase with an IC50 of 8 nM, while being inactive against aldehyde reductase (IC50>100 microM), a related enzyme involved in the detoxification of reactive aldehydes.
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https://www.hal.inserm.fr/inserm-00384538
Contributor : Maité Peney <>
Submitted on : Friday, May 15, 2009 - 1:50:16 PM
Last modification on : Thursday, April 23, 2020 - 2:26:26 PM

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Michael van Zandt, Brian Doan, Diane Sawicki, Janet Sredy, Alberto Podjarny. Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2009, 19 (7), pp.2006-8. ⟨10.1016/j.bmcl.2009.02.037⟩. ⟨inserm-00384538⟩

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