1. Academic Validation
  2. AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey

AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey

  • Bioorg Med Chem Lett. 2004 Sep 6;14(17):4525-8. doi: 10.1016/j.bmcl.2004.06.037.
Robert D Selliah 1 Mark R Hellberg Najam A Sharif Marsha A McLaughlin Gary W Williams Daniel A Scott David Earnest Karen S Haggard W Dennis Dean Pete Delgado Michael S Gaines Raymond E Conrow Peter G Klimko
Affiliations

Affiliation

  • 1 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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