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已发表论文

新型用于抗炎症制剂的吲哚 -2- 酮和 7- 氮杂 -2- 羟基吲哚衍生物的合成与生物评估

 

Authors Chen G, Jiang L, Dong L, Wang Z, Xu F, Ding T, Fu L, Fang Q, Liu Z, Shan X, Liang G

Published Date October 2014 Volume 2014:8 Pages 1869—1892

DOI http://dx.doi.org/10.2147/DDDT.S65997

Received 11 April 2014, Accepted 20 May 2014, Published 13 October 2014

Abstract: Sepsis, a typically acute inflammatory disease, is the biggest cause of death in ICU (intensive care unit). Novel anti-inflammatory alternatives are still in urgent need. In this study, we designed and synthesized 30 indole-2-one and 7-aza-2-oxindole derivatives based on the skeleton of tenidap, and their anti-inflammatory activity was determined by evaluating the inhibitory potency against lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α and interleukin (IL)-6 release in RAW264.7 macrophages. Quantitative SAR (structure–activity relationship) analysis revealed that a high molecular polarizability and low lipid/water partition coefficient (ALogP) in indole-2-one are beneficial for anti-inflammatory activity. Moreover, compounds 7i and 8e inhibited the expression of TNF-α, IL-6, COX-2, PGES, and iNOS in LPS-stimulated macrophages, and 7i exhibited a significant protection from LPS-induced septic death in mouse models. These data present a series of new indole-2-one compounds with potential therapeutic effects in acute inflammatory diseases.
Keywords: anti-inflammation, macrophages, sepsis


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