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

被引：10

作者：

Selliah, RD ^{[1
]}

Hellberg, MR ^{[1
]}

Sharif, NA ^{[1
]}

McLaughlin, MA ^{[1
]}

Williams, GW ^{[1
]}

Scott, DA ^{[1
]}

Earnest, D ^{[1
]}

Haggard, KS ^{[1
]}

Dean, WD ^{[1
]}

Delgado, P ^{[1
]}

Gaines, MS ^{[1
]}

Conrow, RE ^{[1
]}

Klimko, PG ^{[1
]}

机构：

[1] Alcon Res Ltd, Pharmaceut Prod Res, Ft Worth, TX 76134 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 17期

关键词：

11-oxa prostaglandin; glaucoma;

D O I：

10.1016/j.bmcl.2004.06.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4525 / 4528

页数：4

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