局部碳酸酐酶抑制剂

Topical carbonic anhydrase inhibitors.

作者信息

Schoenwald R D, Eller M G, Dixson J A, Barfknecht C F

出版信息

J Med Chem. 1984 Jun;27(6):810-2. doi: 10.1021/jm00372a020.

Abstract

Ethoxzolamide and several derivatives (1-6) were synthesized and evaluated for carbonic anhydrase inhibition (CAI), solubility, pKa, distribution, and corneal permeability. The 6-hydroxy (5) and, particularly, the 6-chloro (6) analogues have the best combination of properties for penetrating the site of action and reducing intraocular pressure. Both 5 and 6 exhibited topical effectiveness in the normal rabbit, with 6 showing greater potency.

摘要

合成了乙氧唑胺及其几种衍生物（1-6），并对其碳酸酐酶抑制作用（CAI）、溶解度、pKa、分布和角膜通透性进行了评估。6-羟基（5），特别是6-氯（6）类似物在穿透作用部位和降低眼压方面具有最佳的性能组合。5和6在正常兔中均表现出局部有效性，其中6的效力更强。