New derivatives of N-[(phenoxy)alkyl]- and N-[(phenoxy)ethoxyethyl]aminoalkanols have been synthesized and evaluated for their anticonvulsant activity in maximal electroshock (MES), maximal electroshock seizure threshold (MEST), and pentylenetetrazol (PTZ) tests. Their neurotoxicity was evaluated via rotarod and chimney tests. The compounds exhibiting the most beneficial activity and protection indices were evaluated for analgesic activity using the formalin test for neurogenic pain. They were also evaluated for their influence on cytotoxic activity using in vitro cellular models (HepG2 and CRL-2534 cell lines). Experiments performed using MTT and neutral red cytotoxicity assays showed that all evaluated compounds were safe for normal, glial cells (astrocytes) and did not induce hepatotoxic effects. Based on the results from the in vitro studies, the safety of the evaluated compounds was inferred. The most promising compound in this research was 1-{2-[2-(2,3-dimethylphenoxy)ethoxy]ethyl}piperidin-3-ol hydrochloride. Additionally, in silico metabolism prediction for the compound has been performed.

中文翻译：

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新型 N-[(苯氧基)烷基]-和 N-[(苯氧基)乙氧基乙基]氨基链烷醇的设计、合成和抗惊厥-镇痛活性†‡

合成了N -[(苯氧基)烷基]-和N -[(苯氧基)乙氧基乙基]氨基烷醇的新衍生物，并评估了它们在最大电休克 (MES)、最大电休克发作阈值 (MEST) 和戊四唑 (PTZ) 中的抗惊厥活性) 测试。通过旋转棒和烟囱试验评估它们的神经毒性。使用福尔马林对神经源性疼痛的测试评估了表现出最有益活性和保护指数的化合物的镇痛活性。还使用体外评估了它们对细胞毒活性的影响细胞模型（HepG2 和 CRL-2534 细胞系）。使用 MTT 和中性红细胞毒性测定进行的实验表明，所有评估的化合物对正常的神经胶质细胞（星形胶质细胞）都是安全的，并且不会引起肝毒性作用。根据体外研究的结果，推断出所评估化合物的安全性。本研究中最有希望的化合物是 1-{2-[2-(2,3-二甲基苯氧基)乙氧基]乙基}哌啶-3-醇盐酸盐。此外，已经对该化合物进行了计算机代谢预测。