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

Article Details

Citation

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

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.

PubMed ID
15357985 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
LatanoprostProstaglandin F2-alpha receptorEC 50 (nM)34.4N/AN/ADetails