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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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Published in: | Bioorganic & medicinal chemistry letters 2004-09, Vol.14 (17), p.4525-4528 |
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Main Authors: | , , , , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2004.06.037 |