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Synthetic Transformations of Higher Terpenoids. 39.∗ Synthesis and Analgesic Activity of Isopimaric Acid Derivatives
Chemistry of Natural Compounds ( IF 0.8 ) Pub Date : 2021-05-28 , DOI: 10.1007/s10600-021-03391-1
M. A. Gromova , Yu. V. Kharitonov , S. A. Borisov , D. S. Baev , T. G. Tolstikova , E. E. Shul’ts

New derivatives of isopimaric acid at the carboxylic acid were prepared. Their analgesic activity was studied in models of visceral and thermal pain. Isopimaric acid amides with aminoethanol and (2R)-(hydroxymethyl)pyrrolidine groups exhibited statistically significant analgesic activity in acetic acid-induced writhing (5 and 25 mg/kg doses) and hot-plate tests (25 mg/kg dose) that was comparable to that of diclofenac sodium (10 mg/kg dose). The new agents were characterized by low (LD50 > 1250 mg/kg) in vivo toxicity. Molecular modeling of possible interaction of the most active compounds with transmembrane G-protein-binding cannabinoid receptor CB2 was performed.



中文翻译:

高级萜类化合物的合成转化。39.*异海松酸衍生物的合成及镇痛活性

制备了异海松酸羧酸的新衍生物。在内脏痛和热痛模型中研究了它们的镇痛活性。异海松酸酰胺与氨基乙醇和 (2 R )-(羟甲基)吡咯烷组在乙酸诱导的扭体(5 和 25 mg/kg 剂量)和热板试验(25 mg/kg 剂量)中表现出统计学上显着的镇痛活性。与双氯芬酸钠(10 mg/kg 剂量)相当。新药剂的特点是体内毒性低(LD 50 > 1250 mg/kg)。对最活跃的化合物与跨膜 G 蛋白结合大麻素受体 CB 2的可能相互作用进行了分子建模。

更新日期:2021-05-28
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