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Synthesis and Antiepileptic Activity Evaluation of Valproic Acid Derivatives by Niche Chemistry

机译:利基化学对丙甲酸衍生物的合成与抗癫痫酸衍生物

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In order to prepare new antiepileptic drugs with a broader clinical application and lower toxic side effects, we have employed esterification and condensation reactions (we call it Niche Chemistry) to reduce the use of valproic acid as the target molecule. In combination with the study of a broad‐spectrum of novel anticonvulsants, we have synthesized two valeric acid derivative compounds [(4‐acetamidophenyl 2‐propylvalerate (1), and (E)‐5‐(4‐((2‐propylpentanoyl)oxy)styryl)‐1,3‐phenylene bis(2‐propylvalerate) (2) by an esterification reaction. The maximum shock seizure test for products 1 and 2 has been successfully carried out, and their cytotoxic activity and survival effects have also been carefully investigated.
机译:为了用更广泛的临床应用和较低的毒性副作用制备新的抗癫痫药物,我们使用酯化和缩合反应(我们称之为利基化学)以减少丙戊酸作为靶分子的使用。结合研究广谱新的抗惊厥药,我们合成了两个valeric酸衍生物化合物[(4-乙酰氨基苯基2-丙基vale(1),和(e)-5-(4 - ((2-丙基戊酰基)通过酯化反应氧化氧基氧基氢)-1,3-亚苯基双(2)。产品1和2的最大冲击癫痫试验已经成功进行,其细胞毒性活性和生存效应也在仔细调查。

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