title: New ethacrynic acid derivatives as potent cytoskeletal modulators in trabecular meshwork cells.
abstract: 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.
authors.affiliation: Research and Development Center, Santen Pharmaceutical Co. Ltd., Takayama, Ikoma, Japan. shimazaki@snaten.co.jp
authors.forename: Atsushi
authors.initials: A
authors.lastname: Shimazaki
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Suhara
authors.forename: Masaki
authors.initials: M
authors.lastname: Ichikawa
authors.forename: Takeshi
authors.initials: T
authors.lastname: Matsugi
authors.forename: Koji
authors.initials: K
authors.lastname: Konomi
authors.forename: Yasutaka
authors.initials: Y
authors.lastname: Takagi
authors.forename: Hideaki
authors.initials: H
authors.lastname: Hara
authors.forename: Ponugoti Vasantha
authors.initials: PV
authors.lastname: Rao
authors.forename: David Lee
authors.initials: DL
authors.lastname: Epstein
mesh_terms: D000818:Animals; D002417:Cattle; D002478:Cells, Cultured; D003599:Cytoskeleton / Q000187:drug effects* / Q000502:physiology; D004976:Ethacrynic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D014129:Trabecular Meshwork / Q000187:drug effects* / Q000502:physiology
chemical_list: D004976:Ethacrynic Acid