Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives

J DeRuiter, AN Brubaker, WL Whitmer…

Index: DeRuiter; Brubaker; Whitmer; Stein Jr. Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 2024 - 2028

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Citation Number: 42

Abstract

A number of 2-oxoquinoline-1-alkanoic acids that contain the N-acylglycine fragment found in several known inhibitors of aldose reductase were synthesized and tested in the rat lens assay. All of the target compounds were prepared by alkylation of the appropriate 2- oxoquinoline intermediates with a halo ester, followed by hydrolysis of the intermediate esters. In the rat lens assay, the 1-acetic acid derivatives 9a-e display the highest level of ...