.alpha.-(1,3-dicarbonylenol ether) methyl ketones as cysteine pr

Details .alpha.-(1,3-dicarbonylenol ether) methyl ketones as cysteine pr .alpha.-(1,3-dicarbonylenol ether) methyl ketones as cysteine pr

1995-06-07

1998-02-03

Shah, Mukuno J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514459, 514460, 514471, 544149, 544152, 549292, 549318, 549417, C07D25300, C07D40900, A61K 31535, A61K 3700

Patent

active

057144842

ABSTRACT:
Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly 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 .beta.-dicarbonyl enol ether leaving group.

REFERENCES:
patent: 4518528 (1985-05-01), Rasnick
patent: 5055451 (1991-10-01), Krantz et al.
patent: 5158936 (1992-10-01), Krantz et al.
patent: 5462939 (1995-10-01), Dolle et al.
patent: 5486623 (1996-01-01), Zimmerman et al.
patent: 5585486 (1996-12-01), Dolle et al.
Chemical Abstract 120:135102 (1993).
Chemical Abstract 113:2570 (1989).
Chemical Abstract 78:43256 (1972).

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