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

Graphic 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 intraocu...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4525-4528
Main Authors: Selliah, Robert D, Hellberg, Mark R, Sharif, Najam A, McLaughlin, Marsha A, Williams, Gary W, Scott, Daniel A, Earnest, David, Haggard, Karen S, Dennis Dean, W, Delgado, Pete, Gaines, Michael S, Conrow, Raymond E, Klimko, Peter G
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Language:English
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Summary:Graphic 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2004.06.037