New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells.
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.
Shimazaki, A; Suhara, H; Ichikawa, M; Matsugi, T; Konomi, K; Takagi, Y; Hara, H; Rao, PV; Epstein, DL
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