Thiadiazole compounds useful as inhibitors of cysteine activity

Details Thiadiazole compounds useful as inhibitors of cysteine activity Thiadiazole compounds useful as inhibitors of cysteine activity

1998-03-02

2000-12-19

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514361, 548128, 548130, A61K 3141, C07D28568

Patent

active

061627917

ABSTRACT:
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): ##STR1## where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.

REFERENCES:
patent: 5036085 (1991-07-01), Heinemann

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