新型抗炎酸基咪唑盐的合成

Q3 Chemistry European Chemical Bulletin Pub Date : 2021-01-01 DOI:10.17628/ecb.2021.10.67-72
T. Somasekhar, Monisha Javadi, R. Sistla, U. Mallavadhani
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引用次数: 1

摘要

采用两步法合成了10种新型的usic酸基咪唑盐。新合成的化合物在体外对U937细胞分泌的细胞因子蛋白TNF- α和IL - 1 β的抗炎潜力进行了评估。部分咪唑盐对TNF- α和IL - 1β具有良好的抗炎活性,其IC 50值在5.3 μM ~ 7.5 μM之间,比母体化合物(> ~ 100 μM)低许多倍。最重要的是,在咪唑盐中与电负性基团的取代被发现更有效,并表现出增强的抗炎活性。
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Synthesis of novel anti-inflammatory usnic acid-based imidazolium salts
Ten novel usnic acid based imidazolium salts were synthesized by employing a two-step protocol. The anti-inflammatory potential of the newly synthesised compounds was evaluated in vitro against cytokine proteins TNF- α and IL - 1 β secreted from U937 cells. Some of the imidazolium salts exhibited promising anti-inflammatory activity against the TNF- α and IL - 1β with IC 50 values ranging between 5.3 μM - 7.5 μM, which are many folds lower than that of the parent compound (>100 μM). Most significantly, substitution with electronegative groups in imidazolium salts of usnic acid found to be more potent and exhibiting enhanced anti-inflammatory activity.
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European Chemical Bulletin
European Chemical Bulletin Chemistry-Chemistry (all)
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