Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides
作者:Kenneth L. Shepard、Samuel L. Graham、Ronald J. Hudcosky、Stuart R. Michelson、Thomas H. Scholz、Harvey Schwam、Anthony M. Smith、John M. Sondey、Kim M. Strohmaier
DOI:10.1021/jm00114a020
日期:1991.10
active carbonic anhydrase inhibitor. Recent results from several research groups indicate that considerable progress has been made toward this objective. In this report, we present the design and synthesis of (hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the
几十年来,治疗原发性开角型青光眼的诱人目标一直是开发局部活性的碳酸酐酶抑制剂。几个研究小组的最新结果表明,朝着这个目标已经取得了相当大的进步。在这份报告中,我们介绍了(羟烷基)磺酰基取代的苯-和噻吩磺酰胺的设计和合成。在局部滴注后,这些化合物在纳摩尔浓度范围内表现出对碳酸酐酶II的抑制作用,并且在经α-胰凝乳蛋白酶处理的高眼压性高血压兔模型中具有较低的眼内压。