Substitution of a 4-biaryl piperidine sulfonamide core , which binds at the S1 ' subsite of MMP-3 , was optimised to give potent inhibitors of MMP-3 , with greater than 300-fold selectivity over MMP-1 , MMP-2 , MMP-9 and MMP-14.
A series of novel , MMP-1 sparing arylhydroxamate sulfonamides with activity against MMP-2 and -13 is described.
A novel series of diazepine-based hydroxamic acid inhibitors of MMP-1 , MMP-9 , and MMP-13 were prepared and evaluated both in vitro and in vivo.
Synthesis and activity of a series of 4-thiazol-yl substituted analogs of novel pyrrolocarbazole 1 as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors have been disclosed.
Poly (ADP-ribose) polymerase-1 (PARP-1 , EC) , a nuclear enzyme activated by DNA strand breaks , physiologically participates in DNA repair.