Phenyl-Substituted Prostaglandins: Potent and Selective Antiglaucoma Agents

Article abstract of DOI:10.1021/jm00054a008

A series of phenyl-substituted analoques of prostaglandin F_2α (PGF_2α) were prepared and evaluated for ocular hypotensive effect and side effects in different animal models.In addition, the activity of the analogues on FP receptors was studied in vitro.The results were compared with those of PGF_2α and its isopropyl ester.The phenyl-substituted PGF_2α analogues exhibited good intraocular pressure reducing effect, were more selective, and exhibited a much higher therapeutic index in the eye than PGF_2α or its isopropyl ester.The analogues exhibited high activity on FP receptors in a stereoselective manner for the 15_a-hydroxyl group.