Cerebrovasodilatation through selective inhibition of the enzyme carbonic anhydrase. 1. Substituted benzenedisulfonamides
作者:Peter E. Cross、Brian Gadsby、Gerald F. Holland、William M. McLamore
DOI:10.1021/jm00207a001
日期:1978.9
A series of substituted benzenedisulfonamide carbonic anhydrase inhibitors is described and their anticonvulsant activities are listed. One compound, 4-(4-methoxypiperidinosulfonyl)-2-chlorobenzenesulfonamide (19, UK-12130), was found to have anticonvulsant activity in animals at a dose level that gave only a minimal diuretic effect. 19 selectively increased cerebral blood flow in animals and man without
描述了一系列取代的苯二磺酰胺碳酸酐酶抑制剂,并列出了它们的抗惊厥活性。发现一种化合物4-(4-甲氧基哌啶子基磺酰基)-2-氯苯磺酰胺(19,UK-12130)在动物中具有抗惊厥活性,其剂量水平仅产生最小的利尿作用。19选择性地增加了动物和人类的脑血流量,却没有产生不可接受的代谢性酸中毒水平。