Alkenoic acid compounds for mechanism-based inactivation of dehy

Details Alkenoic acid compounds for mechanism-based inactivation of dehy Alkenoic acid compounds for mechanism-based inactivation of dehy

1992-01-28

1993-08-24

Naff, David M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514744, 435184, C12N 999, A01N 2902, A01N 4300

Patent

active

052389308

ABSTRACT:
Alkenoic acid compounds are described. The compounds which are dehydropeptidase inactivators contain a ##STR1## moiety which is substituted with a halomethylene or a cyano moiety as R.sub.3. The enzyme deprotonates the alpha--CH.sub.2 group and then the intermediate compound forms a covalent bond with enzymic residue in the active site, resulting in irreversible inactivation of the enzyme. The compounds are particularly inactivators of renal dipeptidases.

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