A series of novel cinnamoylpiperazine derivatives (5a–5l) were synthesized as potential antinociceptive, and anticonvulsive agents. Various heterocyclic systems like piperidine, morpholine, piperazine, and N-arylpiperazine were combined with cinnamoyl or methylenedioxy cinnamoyl moieties to obtain a series of constrained analogs of cinnamides. Of these, compound 5e possessing 4-fluorophenyl substitution on the piperazine ring exhibited good antinociceptive activity in capsaicin and formalin-induced nociception methods, and also significant anticonvulsant activity in pentylenetetrazole and maximal electroshock-induced seizure methods. Further, all the derivatives were studied for molecular and preadmet properties. The activities of compound 5e were supported by molecular and preadmet properties for its in silico oral bioavailability and drug-likeness.

中文翻译：

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取代的肉桂酰基哌嗪衍生物作为潜在的抗伤害药和抗惊厥药的合成，评价和分子性质预测

合成了一系列新颖的肉桂酰基哌嗪衍生物（5a - 5l），作为潜在的抗伤害药和抗惊厥药。将各种杂环系统（例如哌啶，吗啉，哌嗪和N-芳基哌嗪）与肉桂酰基或亚甲基二氧基肉桂酰基部分结合，以获得一系列约束的肉桂酸酯类似物。其中，在哌嗪环上具有4-氟苯基取代的化合物5e在辣椒素和福尔马林诱导的伤害感受方法中表现出良好的抗伤害感受活性，在戊四氮和最大电击诱发癫痫发作方法中表现出显着的抗惊厥活性。此外，研究了所有衍生物的分子和前卫性质。化合物5e的活性 其分子内口服生物利用度和药物相似性受到分子和前导物性质的支持。