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

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

Bioorg Med Chem Lett

Dipartimento Farmaco-chimico, Faculty of Pharmacy, University of Messina, Polo Universitario Annunziata, 98168 Messina, Italy.

Published: January 2011

AI Article Synopsis

Article Abstract

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 IC(50) values very similar to that of epalrestat, the only ARI currently used in therapy.

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Source
http://dx.doi.org/10.1016/j.bmcl.2010.11.041DOI Listing

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