ChemInform Abstract: Synthesis and Biological Activity of Aldose Reductase Inhibitors with Michael Acceptor Substituents

Autor:	Anita Bartoszko-Malik, Duane D. Miller, Yasar S. Abdel‐Ghany, Tadashi Mizoguchi, Isaac O. Donkor, Peter F. Kador
Rok vydání:	2010
Předmět:	Aldose reductase chemistry.chemical_compound Rat lens chemistry Stereochemistry Alrestatin Michael reaction Rat kidney Biological activity General Medicine Aldehyde Reductase
Zdroj:	ChemInform. 30
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.199934174
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::5b79b0375f0d1343a98be83bb989d6dc https://doi.org/10.1002/chin.199934174 Zobrazit plný text záznamu Plný text