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    Synthesis and use of &agr;-ketoamide derivatives and arrays
    10.
    发明授权
    Synthesis and use of &agr;-ketoamide derivatives and arrays 失效
    α-酮酰胺衍生物和阵列的合成和应用

    公开(公告)号：US06452050B1

    公开(公告)日：2002-09-17

    申请号：US09531737

    申请日：2000-03-21

    申请人： Carmen M. Baldino ,  David L. Coffen ,  Stewart D. Chipman ,  Hong Cheng

    发明人： Carmen M. Baldino ,  David L. Coffen ,  Stewart D. Chipman ,  Hong Cheng

    IPC分类号： C07C23307

    CPC分类号： C40B40/04 ,  C07C275/40 ,  C07C335/20 ,  C07D333/60

    摘要： The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.

    摘要翻译： 本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。 这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。 新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000个α-酮酰胺衍生物，具有针对三个半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物 通过本文所述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药剂。 虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。