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设计和合成 2-(1,3-二氧代异吲哚啉-2-基)-N-(4-氧代-2-取代噻唑烷-3-基)乙酰胺衍生物作为潜在的抗惊厥药物。

Design and synthesis of 2-(1, 3-dioxoisoindolin-2-yl)-N-(4-oxo-2-substitutedthiazolidin-3-yl) acetamide derivatives as potential anticonvulsant agents.

机构信息

Department of Pharmaceutical Chemistry, YB Chavan College of Pharmacy, Dr Rafiq Zakaria Campus, Rauza Bagh, PB No 33, Aurangabad, Maharashtra 431001, India.

出版信息

Eur J Med Chem. 2011 Nov;46(11):5448-55. doi: 10.1016/j.ejmech.2011.09.003. Epub 2011 Sep 8.

Abstract

A series of 2-(1,3-dioxoisoindolin-2-yl)-N-(4-oxo-2-substitutedthiazolidin-3-yl) acetamide derivatives were designed and synthesized using appropriate synthetic route, keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS depressant activities in mice. The synthesized derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (sc-PTZ) induced seizure and neurotoxicity screens and were also evaluated for behavioral activity. All the tested compounds showed protection against MES test indicative of their ability to inhibit the seizure spread.

摘要

设计并合成了一系列 2-(1,3-二氧代异吲哚啉-2-基)-N-(4-氧代-2-取代噻唑烷-3-基)乙酰胺衍生物,考虑到药效团的结构要求,并在小鼠中评估了它们的抗惊厥和中枢神经抑制剂活性。在最大电休克(MES)、皮下戊四氮(sc-PTZ)诱导的惊厥和神经毒性筛选中对合成的衍生物进行了检测,并对其行为活性进行了评估。所有测试的化合物都显示出对 MES 测试的保护作用,表明它们具有抑制癫痫发作传播的能力。

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