Synthesis and use of .alpha.-ketoamide derivatives and arrays

Details Synthesis and use of .alpha.-ketoamide derivatives and arrays Synthesis and use of .alpha.-ketoamide derivatives and arrays

1998-04-16

2000-11-07

Lukton, David

Organic compounds -- part of the class 532-570 series

Organic compounds

Amino nitrogen containing

568305, 568306, 564502, 514 19, 530332, C07C23300

Patent

active

061439312

ABSTRACT:
The invention is based on new methods for making and using compounds and arrays of novel .alpha.-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 .alpha.-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 pharmaceutic 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.

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Bergman et al., "Studies of the Reaction Between Indole-2,3-diones (Isatins) and Secondary Aliphatic Amines", ACTA Chemica Scnandinavica, 51: 753-759 (1997).
Bergman et al., "Synthesis of 5H-Pyrazino[2,3-b]indoles from Indole-2,3-dione Derivatives", ACTA Chemica Scandinavic, 51:742-752 (1997) .

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