PHENYL-SUBSTITUTED PROSTAGLANDINS - POTENT AND SELECTIVE ANTIGLAUCOMA AGENTS

被引：136

作者：

RESUL, B ^{[1
]}

STJERNSCHANTZ, J ^{[1
]}

NO, KY ^{[1
]}

LILJEBRIS, C ^{[1
]}

SELEN, G ^{[1
]}

ASTIN, M ^{[1
]}

KARLSSON, M ^{[1
]}

BITO, LZ ^{[1
]}

机构：

[1] COLUMBIA UNIV COLL PHYS & SURG,DEPT OPHTHALMOL,NEW YORK,NY 10032

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 02期

关键词：

D O I：

10.1021/jm00054a008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of phenyl-substituted analogues of prostaglandin F2alpha (PGF2alpha) were prepared and evaluated for ocular hypotensive effect and side effects in different animal models. In addition, the activity of the analogues on FP receptors was studied in vitro. The results were compared with those of PGF2alpha and its isopropyl ester. The phenyl-substituted PGF2alpha analogues exhibited good intraocular pressure reducing effect, were more selective, and exhibited a much higher therapeutic index in the eye than PGF2alpha or its isopropyl ester. The analogues exhibited high activity on FP receptors in a stereoselective manner for the 15alpha-hydroxyl group.

引用

页码：243 / 248

页数：6

共 30 条

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