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.

Metalloenzyme inhibitors with clinical potential: Derivatives of 1-hydroxypiperazino-2,6-dione as a new ligation group for zinc

ROSSELLO, ARMANDO;
2008

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/600467
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