The present invention pertains to new compds. having increased capacity for inhibiting metalloproteinases contg. zinc at the active center. The inhibitors here disclosed possess a new type of chelating group for the zinc(II) ion at the enzymic catalytic center: a heterocycle with a 6-member ring, 1-hydroxypiperazino-2,6-dione. These compds. can be derived from an iminodiacetic acid or other amino acids contg. or not chiral centers with one or more C atoms in the ring and possessing adequate lipophilic 4-N-substituents. These new compds. exhibit increased stability and inhibitory activity (of nanomolar order) and selectivity for certain matrix metalloproteinases and thus may have applications in pharmacol.
New Inhibitors of Metalo-enzymes with Potential Clinical Application: 1-hydroxy-piperazino-2,6-dione as a new Zinc-binding group
ROSSELLO, ARMANDO;
2008-01-01
Abstract
The present invention pertains to new compds. having increased capacity for inhibiting metalloproteinases contg. zinc at the active center. The inhibitors here disclosed possess a new type of chelating group for the zinc(II) ion at the enzymic catalytic center: a heterocycle with a 6-member ring, 1-hydroxypiperazino-2,6-dione. These compds. can be derived from an iminodiacetic acid or other amino acids contg. or not chiral centers with one or more C atoms in the ring and possessing adequate lipophilic 4-N-substituents. These new compds. exhibit increased stability and inhibitory activity (of nanomolar order) and selectivity for certain matrix metalloproteinases and thus may have applications in pharmacol.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
