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Synthesis and pharmacological evaluation of novel limonin derivatives as anti-inflammatory and analgesic agents with high water solubility. 2014
Yun Yang, and
Xinhui Wang, and
Qihua Zhu, and
Guoqing Gong, and
Danmeng Luo, and
Aidou Jiang, and
Liyan Yang, and
Yungen Xu
Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing, Jiangsu 21009, China.
A novel series of water-soluble derivatives of limonin were synthesized by introducing various tertiary amines onto the C (7)-position of limonin. Ten target compounds were characterized and screened for their anti-inflammatory and analgesic activity in vivo. Compound 3c exhibited the strongest analgesic and anti-inflammatory activity among the limonin and its derivatives tested; its analgesic activity is more potent than that of aspirin and its anti-inflammatory activity is stronger than that of naproxen.
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