Cysteine protease inhibitors containing heterocyclic leaving gro

Details Cysteine protease inhibitors containing heterocyclic leaving gro Cysteine protease inhibitors containing heterocyclic leaving gro

1997-09-02

1999-07-20

Dees, Jose'G.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548530, 548531, 548541, 548543, 514359, 5142315, 544111, C07D20712, C07D20714, C07D20716, A61K 3141

Patent

active

059257725

ABSTRACT:
A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: --O--Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.

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Chemical Abstract 120:135102 (1993).
Chemical Abstract 113:2570 (1989).
Chemical Abstract 78:43256 (1972).

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