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In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2011)

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 1, 页码 200-203

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.041

关键词

Aldose reductase; Enzyme inhibition; Diabetes complications; 4-Thiazolidinones

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Chemistry, Medicinal Chemistry, Organic

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  1. University of Messina
  2. University of Pisa

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2-Thioxo-4-thiazolidinone derivatives were evaluated as aldose reductase inhibitors (ARIs) and most of them exhibited good or excellent in vitro efficacy. Out of the tested compounds, most N-unsubstituted analogues were found to possess inhibitory effects at low micromolar doses and two of them exhibited higher potency than sorbinil, used as a reference drug. The insertion of an acetic chain on N-3 of the thiazolidinone scaffold led to analogues with submicromolar affinity for ALR2 and IC50 values very similar to that of epalrestat, the only ARI currently used in therapy. (C) 2010 Elsevier Ltd. All rights reserved.

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