文章基本信息

标题：New Ethacrynic Acid Derivatives as Potent Cytoskeletal Modulators in Trabecular Meshwork Cells
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作者：Atsushi Shimazaki ; Hiroshi Suhara ; Masaki Ichikawa 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2004
卷号：27
期号：6
页码：846-850
DOI：10.1248/bpb.27.846
出版社：The Pharmaceutical Society of Japan
摘要：A series of ethacrynic acid (ECA) derivatives were synthesized and examined for ocular hypotensive activity. Efficacy was evaluated in a cell-shape assay, using human trabecular meshwork cells, and cytotoxicity in a (3-(4,5-dimethylthiazole-2-yl)-5-(3-carboxymethoxy phenyl)-2-(4-sulfophenyl)-2 H -tetrazolium) assay, using cultured bovine trabecular meshwork cells. Many of the derivatives demonstrated efficacy equal to or greater than that of ECA. SA9000 was selected as the most promising candidate for a novel ocular hypotensive drug with few side effects.
关键词：ethacrynic acid;trabecular meshwork cell;structure–activity relationship;cell shape;cytoskeletal modulating efficacy;cytotoxicity