Identification of novel plasmin inhibitors possessing nitril moiety as warhead. Bioorg. Med.

Identification of novel plasmin inhibitors possessing nitril moiety as warhead. Bioorg. Med.
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具有腈部分作为弹头的新型纤溶酶抑制剂的鉴定。

DOI:
10.1016/j.bmcl.2011.08.121
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发表时间:
2011
期刊:
Chem. Lett.
影响因子:
--
通讯作者:
Tsuda Y.
Tsuda Y.
中科院分区:
--
文献类型:
--
作者:
Teno N.;Gohda K.;Wanaka K.;Sueda T.;Tsuda Y.

文献摘要

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制备了具有三取代苯的赖氨酸-腈衍生物,其属于新的化学类别,并测试了其对纤溶酶和高度同源的血浆激肽释放酶和尿激酶的抑制活性。新的化学型在纤溶酶抑制剂的开发中的用途已经通过化合物9的衍生物证明。
Lysine-nitrile derivatives having a trisubstituted benzene, which belongs to a new chemical class, were prepared and tested for inhibitory activities against plasmin and the highly homologous plasma kallikrein and urokinase. The use of the novel chemotype in the development of plasmin inhibitors has been demonstrated by derivatives of compound 9.