TOPICALLY ACTIVE CARBONIC-ANHYDRASE INHIBITORS .3. BENZOFURAN-SULFONAMIDE AND INDOLE-2-SULFONAMIDE

被引：53

作者：

GRAHAM, SL ^{[1
]}

HOFFMAN, JM ^{[1
]}

GAUTHERON, P ^{[1
]}

MICHELSON, SR ^{[1
]}

SCHOLZ, TH ^{[1
]}

SCHWAM, H ^{[1
]}

SHEPARD, KL ^{[1
]}

SMITH, AM ^{[1
]}

SMITH, RL ^{[1
]}

SONDEY, JM ^{[1
]}

SUGRUE, MF ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,CTR RECH,RIOM,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 02期

关键词：

D O I：

10.1021/jm00164a045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Derivatives of benzofuran- and indole-2-sulfonamide were prepared for evaluation as topically active ocular hypotensive agents. These compounds were found to be excellent inhibitors of carbonic anhydrase and to lower intraocular pressure in a rabbit model of ocular hypertension. However, the development of these compounds for clinical use was precluded by the observation that they cause dermal sensitization in guinea pigs. A correlation between electrophilicity, as assessed by in vitro reactivity with reduced glutathione, and dermal sensitization potential was further documented. © 1990, American Chemical Society. All rights reserved.

引用

页码：749 / 754

页数：6

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