Design and synthesis of 2-(arylamino)-4 (3H)-quinazolinones as novel inhibitors of rat lens aldose reductase

J DeRuiter, AN Brubaker, J Millen…

文献索引：DeRuiter; Brubaker; Millen; Riley Journal of Medicinal Chemistry, 1986 , vol. 29, # 5 p. 627 - 629

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被引用次数: 39

摘要

A number of 2-(arylamino)-4 (3H)-quinazolinones (2a-i) that possess several of the pharmacophore moieties necessary for binding to the inhibitor site of the enzyme aldose reductase were synthesized and tested for their ability to inhibit crude aldose reductase obtained from rat lens. Only those quinazolinones that possess an acidic moiety on the 2- (arylamino) substituent were found to display significant inhibitory activity. Of these, the ...