β-萘结合噻唑-5-羧胺类/噻唑-5-酮类:设计、合成及抗惊厥药物筛选

M. Arshad, F. Al-Otaibi, G. Mustafa, S. Shousha, A. Alshahrani
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引用次数: 0

摘要

利用4-甲基-2-(萘-2-基)噻唑-5-羰基氯与适当的胺反应,制备了一组β-萘掺入噻唑-5-羧酰胺/噻唑-5-酮(7a- 70和8a-8e)。所有化合物的结构均通过元素分析、FT-IR、1H NMR和质谱数据进行了解释。采用MES和化学休克(scPTZ)发作试验评估化合物的抗惊厥活性。还评估了神经毒性。这些化合物大多数对两种动物模型都有显著的活性;化合物7e, 7j, 7n和8c显示出良好的活性,可以作为进一步研究的线索。
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β-Naphthalene Incorporated Thiazole-5-Carboxamides/Thiazole -5- Ketones: Design, Synthesis and Anticonvulsant Screening against Two Seizure Models
A bunch of β-naphthalene incorporated thiazole-5-carboxamides/thiazole -5- ketones (7a-7o& 8a-8e) were prepared by reacting 4-methyl-2-(naphthalen-2-yl)thiazole-5-carbonyl chloride with appropriate amines. Structures of all the compounds were explained by elemental analysis, FT-IR, 1H NMR and mass spectral data. The compounds were evaluated for their anticonvulsant activity employing MES and chemoshock (scPTZ) seizure tests. Neurotoxicity was also assessed. Majority of these compounds exhibited significant activity against both animal models; however, compounds 7e, 7j, 7n and 8c displayed promising activity and could be considered as leads for further investigations.
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