Enzyme Systems Products

Other

Prototek, Inc.

David W Rasnick

Kyujin Cho

Eugene R Bissell

Novel &agr;-amino and peptidyl sulfonyl imidazolides, a method for their synthesis, and a method for inhibiting serine proteases therewith are disclosed. Pharmaceutical compositions containing &agr;-amino and peptidyl sulfonyl imidazolides and their use in the treatment of disease states characterized by an over-activity of serine proteases are also disclosed. Novel synthetic methods for the synthesis of sulfonyl derivatives, particularly &agr;-amino and peptidyl sulfonyl derivatives, from thioic acid S-esters are also disclosed.

Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases

Peptide thioneamides are provided as synthetic substrates for cysteine proteases. The compounds of the invention are peptides consisting of one or more blocked or unblocked amino acids wherein the terminal carboxy of the peptides are thionated and forms a thioneamide linkage with a fluorogenic or chromogenic leaving group. The alpha carbonyls of the remaining amino acids are thionated or unthionated. The invention includes methods and kits for using the peptide thioneamides.

Method of detecting cysteine proteases

Peptide thioneamides are provided as synthetic substrates for cysteine proteases. The compounds of the invention are peptides consisting of one or more blocked or unblocked amino acids wherein the terminal carboxy of the peptides are thionated and forms a thioneamide linkage with a fluorogenic or chromogenic leaving group. The alpha conbonyls of the remaining amino acids are thionated or unthionated. The invention includes methods and kits for using the peptide thioneamides.

Peptide thioneamides as selective substrates for cysteine proteases

Novel .alpha. amino fluoro ketones, a method of their synthesis and a method for irreversibly inhibiting proteases is disclosed.

.alpha. Amino fluoro ketones

Substrates and their corresponding pharmaceutically acceptable acid salts derived from 7-amino-4-trifluoromethyl-quinolone are disclosed. These substrates are useful for determining the presence of an enzyme or enzyme inhibitor in a biological fluid, wherein the fluid is contacted with a substrate. This mixture is thereafter incubated to effect enzymatic hydrolysis. Subsequently, the presence of the free 7-amino-4-trifluoro-methylquinolone is fluorometrically detected.

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Sunol, CA, United States of America

David W Rasnick