New Ethacrynic Acid Derivatives as Potent Cytoskeletal Modulators in Trabecular Meshwork Cells

Atsushi Shimazaki; Hiroshi Suhara; Masaki Ichikawa; Takeshi Matsugi; Koji Konomi; Yasutaka Takagi; Hideaki Hara; Ponugoti Vasantha Rao; David Lee Epstein

doi:10.1248/bpb.27.846

Regular Articles

New Ethacrynic Acid Derivatives as Potent Cytoskeletal Modulators in Trabecular Meshwork Cells

Atsushi Shimazaki, Hiroshi Suhara, Masaki Ichikawa, Takeshi Matsugi, Koji Konomi, Yasutaka Takagi, Hideaki Hara, Ponugoti Vasantha Rao, David Lee Epstein

著者情報

キーワード: ethacrynic acid, trabecular meshwork cell, structure–activity relationship, cell shape, cytoskeletal modulating efficacy, cytotoxicity

ジャーナルフリー

2004 年 27 巻 6 号 p. 846-850

DOI https://doi.org/10.1248/bpb.27.846

詳細

抄録

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)-2H-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.

責任著者(Corresponding author)

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