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AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey |
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| Authors: | Selliah Robert D Hellberg Mark R Sharif Najam A McLaughlin Marsha A Williams Gary W Scott Daniel A Earnest David Haggard Karen S Dean W Dennis Delgado Pete Gaines Michael S Conrow Raymond E Klimko Peter G |
| Institution: | Alcon Research, Ltd, Pharmaceutical Products Research, 6201 South Freeway, MS R2-39 Fort Worth, TX 76134, USA. |
| Abstract: | A series of 11-oxa prostaglandin analogs was evaluated for FP receptor binding and activation. Several compounds having aryloxy-terminated lower chains were found to be potent agonists. Topical ocular dosing of AL-12182, the isopropyl ester prodrug of the potent agonist 13, lowered intraocular pressure in the monkey by 40% accompanied by minimal conjunctival hyperemia in the rabbit. AL-12182 was synthesized on multigram scale starting with D-sorbitol. |
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