Novel series of limonin derivatives （V-A-I-V-A-8, V-B-I-V-B-8） were synthesized by adding various tertiary amines onto the C （7）-position of limonin. The synthesized compounds possessed favorable physicochemical p...Novel series of limonin derivatives （V-A-I-V-A-8, V-B-I-V-B-8） were synthesized by adding various tertiary amines onto the C （7）-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.展开更多
基金supported by the National Natural Science Foundation of China(Grant No.21472242)the National Science and Technology Major Project for "Significant New Drugs Creation" of China(Grant No.2015ZX09102001)State Key Laboratory of Natural Medicines,China Pharmaceutical University(No.SKLNMZZCX201406)
文摘Novel series of limonin derivatives （V-A-I-V-A-8, V-B-I-V-B-8） were synthesized by adding various tertiary amines onto the C （7）-position of limonin. The synthesized compounds possessed favorable physicochemical property, and the intrinsic solubility of the novel compounds were significantly improved, compared with limonin. Different pharmacological models were used to evaluate the analgesic and anti-inflammatory activities of the target compounds. Compound V-A-8 exhibited the strongest in vivo activity among the novel limonin analogs; its analgesic activity was more potent than aspirin and its anti-inflammatory activity was stronger than naproxen under our testing conditions.
