Title: Synthesis and biological activity of aldose reductase inhibitors with Michael acceptor substituents
Abstract: Derivatives of alrestatin (1–5) and alconil (6–8) possessing Michael acceptor substituents were synthesized as aldose reductase inhibitors. The alrestatin derivatives demonstrated enhanced aldose reductase inhibitory activity. The most potent reversible inhibitor of the series (compound 3) was 15-fold more active than alrestatin. Additionally, lipophilic analogues of alrestatin selectively inhibited rat lens aldose reductase versus rat kidney aldehyde reductase. Unlike alrestatin derivatives, alconil derivatives with similar substituents did not demonstrate significant reversible or irreversible inhibition of aldose reductase.
Publication Year: 1999
Publication Date: 1999-03-01
Language: en
Type: article
Indexed In: ['crossref']
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Cited By Count: 7
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