Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors

…, T Cummons, D Barone, S Ayral-Kaloustian…

文献索引：Zask, Arie; Kaplan, Joshua; Du, XueMei; MacEwan, Gloria; Sandanayaka, Vincent; Eudy, Nancy; Levin, Jeremy; Jin, Guixian; Xu, Jun; Cummons, Terri; Barone, Dauphine; Ayral-Kaloustian, Semiramis; Skotnicki, Jerauld Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 6 p. 1641 - 1645

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被引用次数: 25

摘要

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.