Studies on the synthesis and structure-activity relationships of 5-(3'-indolal)-2-thiohydantoin derivatives as aldose reductase enzyme inhibitors.
A new series of 5-(3'-indolal)-2-thiohydantoin derivatives was synthesized and tested for the ability to inhibit bovine lens aldose reductase (AR) enzyme. The compounds were prepared by condensation of substituted indole-3-aldehyde derivatives with 2-thiohydantoin. The capacity of inhibiting the semi-purified bovine lens enzyme in vitro was observed for several of the compounds tested. One of them was found to be effective in reducing the enzyme activity compared with a corresponding well-known AR inhibitor.
Büyükbingöl
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E
Ankara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara, Turkey.
Süzen
S
S
Klopman
G
G
D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors*; D000818:Animals; D002417:Cattle; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013867:Thiohydantoins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D007211:Indoles; D013867:Thiohydantoins; D000449:Aldehyde Reductase