Cysteine protease inhibitors containing heterocyclic leaving gro

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

1993-12-08

1996-01-23

Tsang, Cecilia

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

544316, 546300, 548532, 549479, 514269, 514345, 514459, 514471, 514460, C07D31500, C07D30702, C07D20700, A61K 3135

Patent

active

054866235

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
Chem. Abst. 120:135102 (1993).
Chem Abst. 113:2570 (1989).
Chem Abst. 78:43256 (1972).

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