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

1994-02-15

Lee, Mary C.

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

Organic compounds

Nitriles

558405, 558442, 560226, 560227, 560230, 562449, 562567, 562577, 546329, 546330, 546335, 546341, 549 77, 549 79, C07C25517, C07C 5703

Patent

active

052868931

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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