Design and synthesis of orally active inhibitors of TNF synthesis as anti-rheumatoid arthritis drugs

…, J Huang, F Chu, E Eugui, A Mirkovich, Y Kim…

Index: Chen, Jian Jeffrey; Dewdney, Nolan; Lin, Xiaohong; Martin, Robert L.; Walker, Keith A. M.; Huang, Jane; Chu, Frances; Eugui, Elsie; Mirkovich, Anna; Kim, Yong; Sarma, Keshab; Arzeno, Humberto; Van Wart, Harold E. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 22 p. 3951 - 3954

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Citation Number: 13

Abstract

A novel series of TNF inhibitors was identified based on the screening of existing MMP inhibitor libraries. Further SAR optimization led to the discovery of a novel lead compound. Its synthesis, efficacy in experimental animal models, and pharmacokinetic data are discussed.