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Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters, derived from natural safrole.

机译:衍生自天然黄樟脑的新型N-酰基芳基azo和等位基因的合成及止痛活性。

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摘要

Anew series of antinociceptive compounds belonging to the N-acylarylhydrazone (NAH) class were synthesized from natural safrole (7). The most analgesic derivative represented by 10f, [(4'-N,N-dimethylaminobenzylidene-3-(3', 4'-methylenedioxyphenyl)propionylhydrazine], was more potent than dipyrone and indomethacin, used as standards. The NAH compounds described herein were structurally planned by molecular hybridization and classical bioisosterism strategies on previously reported analgesic NAH in order to identify the pharmacophoric contribution of the N-acylarylhydrazone moiety and investigate the structure-activity relationship (SAR) in these series.
机译:从天然黄樟脑合成了一系列新的N-酰基芳基hydr(NAH)类抗伤害感受化合物(7)。以10f表示的最止痛衍生物,[(4'-N,N-二甲基氨基苄叉基-3-(3',4'-亚甲基二氧苯基)丙酰肼]]比作为标准品的双嘧啶和消炎痛更有效。我们通过分子杂交和经典生物立体异构策略对先前报道的止痛NAH进行结构规划,以鉴定N-酰基芳基hydr部分的药效学作用并研究这些系列中的构效关系(SAR)。

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