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ID: ALA1137983

Journal: Bioorg Med Chem Lett

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

Authors: Selliah RD, Hellberg MR, Sharif NA, McLaughlin MA, Williams GW, Scott DA, Earnest D, Haggard KS, Dean WD, Delgado P, Gaines MS, Conrow RE, Klimko PG.

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.

CiteXplore: 15357985

DOI: 10.1016/j.bmcl.2004.06.037