Cysteine protease inhibitors containing heterocyclic leaving gro

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

1996-01-22

1997-09-02

Grumbling, Matthew V.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549475, 549476, C07D31500, C07D30702, A61K 3134

Patent

active

056633807

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.

REFERENCES:
patent: 4518528 (1985-05-01), Rasnick
patent: 4959503 (1990-09-01), Connor et al.
patent: 5283158 (1994-02-01), Onodera et al.
patent: 5486623 (1996-01-01), Zimmerman et al.

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