In vitro aldose reductase inhibitory activity of N-aryl-glycine derivatives and their thioisosters.
A series of N-arylglycine derivatives and their thioisosters (1-10) was synthesized and evaluated as in vitro aldose reductase inhibitors. Among these, (6-chloro-1,2,4-benzothiadiazine-1,1-dioxide-3-yl)-2-propanoic acid (5) shows an inhibitory activity (IC50:5.1 microM) comparable to Alrestatin.
Costantino
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Cattedra di Chimica Farmaceutica e Tossicologica della Facoltà di Farmacia, Università di Modena.
Parenti
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Di Bella
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Baraldi
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M
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D005123:Eye / Q000201:enzymology; D006852:Hydrochlorothiazide / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D051381:Rats; D011919:Rats, Inbred Strains
D006852:Hydrochlorothiazide; D000449:Aldehyde Reductase