Author/Authors :
Arie Zask، نويسنده , , Joshua Kaplan، نويسنده , , Xuemei Du، نويسنده , , Gloria MacEwan، نويسنده , , Vincent Sandanayaka، نويسنده , , Nancy Eudy، نويسنده , , Jeremy Levin، نويسنده , , Guixian Jin، نويسنده , , Jun Xu، نويسنده , , Terri Cummons، نويسنده , , Dauphine Barone، نويسنده , , Semiramis Ayral-Kaloustian، نويسنده , , Jerauld Skotnicki، نويسنده ,
Abstract :
Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-α release. Oral activity in the mouse LPS model of TNF-α release was seen. Efficacy in the mouse collagen induced arthritis model was achieved with diazepine 20.
