The present study describes the synthesis of a novel series of thiazolidin-4-one and thiazinan-4-one using 1-(2-aminoethyl)pyrrolidine as amine precursor. All compounds were synthesised by one-pot three component cyclocondensation reaction from the amine, a substituted benzaldehyde and a mercaptocarboxylic acid. The compounds were obtained in moderate to good yields and were identified and characterised by 1H, 13 C, 2 D NMR and GC/MS techniques. The compounds also were screened for their in vitro acetylcholinesterase (AChE) activity in hippocampus and cerebral cortex on Wistar rats. The six most potent compounds have been investigated for their cytotoxicity by cell viability assay of astrocyte primary culture, an important cell of central nervous system. We highlighted two compounds (6a and 6k) that had the lowest IC50 in hippocampus (5.20 and 4.46 µM) and cerebral cortex (7.40 and 6.83 µM). These preliminary and important results could be considered a starting point for the development of new AChE inhibitory agents.

中文翻译：

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由1-（2-氨基乙基）吡咯烷作为乙酰胆碱酯酶抑制剂合成噻唑烷丁-4-酮和噻嗪南-4-酮。

本研究描述了使用1-（2-氨基乙基）吡咯烷作为胺前体合成一系列新的噻唑烷丁-4-酮和噻嗪南-4-酮。通过胺，取代的苯甲醛和巯基羧酸的一锅三组分环缩合反应合成所有化合物。以中等至良好的收率获得了化合物，并通过1 H，13 C，2 D NMR和GC / MS技术对其进行了鉴定和表征。还筛选了这些化合物在Wistar大鼠海马和大脑皮层中的体外乙酰胆碱酯酶（AChE）活性。通过星形胶质细胞原代培养物（中枢神经系统的重要细胞）的细胞生存力测定研究了六种最有效的化合物的细胞毒性。我们重点介绍了海马IC50最低的两种化合物（6a和6k）（5.20和4。46 µM）和大脑皮层（7.40和6.83 µM）。这些初步和重要的结果可以被认为是开发新的AChE抑制剂的起点。