We report here the design and synthesis of a novel series of benzylamines that are potent and selective inhibitors of uPA with promising oral availability in rat. Further evaluation of one representative (ZK824859) of the new structural class showed that this compound lowered clinical scores when dosed in either acute or chronic mouse EAE models, suggesting that uPA inhibitors of this type could be useful for the treatment of multiple sclerosis.

中文翻译：

---

发现选择性尿激酶纤溶酶原激活剂（uPA）抑制剂作为多发性硬化症的潜在治疗方法

我们在这里报告了一系列新的苄胺的设计和合成，这些苄胺是uPA的强效和选择性抑制剂，在大鼠中具有良好的口服有效性。对新结构类别的一名代表（ZK824859）的进一步评估表明，该化合物在急性或慢性小鼠EAE模型中给药时降低了临床评分，表明这种类型的uPA抑制剂可用于治疗多发性硬化症。