Carbonic anhydrase inhibitors: Topically acting antiglaucoma sulfonamides incorporating esters and amides of 3-and 4-carboxybenzolamide

被引：33

作者：

Casini, A

Scozzafava, A

Mincione, F

Menabuoni, L

Starnotti, M

Supuran, CT

机构：

[1] Univ Florence, Lab Chim Inorgan & Bioinorgan, I-50019 Florence, Italy

[2] Osped Pescia, UO Oculist, Pescia, Italy

[3] Casa Cura Villa Donatello, I-50100 Florence, Italy

[4] Clin Oculist, I-50134 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(03)00580-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Reaction of 3- and 4-carboxybenzenesulfonyl chloride with 5-amino-1,3,4-thiadiazole-2-sulfonaniide/5-imino-4-methyl-delta(2)-1,3,4-thiadiazoline-2-sulfonamide afforded two series of benzolamide analogues to which the carboxyl moiety has been derivatized as esters or amides. in order to reduce their very polar character. The new derivatives showed low nanomolar affinity for three carbonic anhydrase (CA) isozymes, CA I, II and IV, and were effective as topical antiglaucoma agents in normotensive rabbits. Efficacy of several of the new sulfonamides reported was better than that of the standard drugs dorzolamide and brinzolamide, whereas their duration of action was prolonged as compared to that of the clinically used drugs. (C) 2003 Elsevier Ltd. All rights reserved.

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页码：2867 / 2873

页数：7

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