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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, antiarrhythmic and anticoagulant activities of novel thiazolo derivatives from methyl 2-(thiazol-2-ylcarbamoyl)acetate.
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Synthesis, antiarrhythmic and anticoagulant activities of novel thiazolo derivatives from methyl 2-(thiazol-2-ylcarbamoyl)acetate.

机译:由2-(噻唑-2-基氨基甲酰基)乙酸甲酯合成新型噻唑并衍生物的抗心律失常和抗凝血活性。

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摘要

A series of novel thiazolo derivatives were synthesized by initial condensation of methyl 2-(thiazol-2-ylcarbamoyl)acetate with phenyl isothiocyanate and further reactions using different organic reagents. The structures of newly synthesized compounds were confirmed by IR, 1H NMR, EIMS spectral data and elemental analysis. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds were screened for their antiarrhythmic and anticoagulant activities and they showed high antiarrhythmic activity compared with procaine amide and lidocaine as positive controls. The detailed synthesis, spectroscopic data, LD(50) and pharmacological activities of the synthesized compounds were reported.
机译:通过2-(噻唑-2-基氨基甲酰基)乙酸甲酯与异硫氰酸苯酯的初始缩合反应,并使用不同的有机试剂进行进一步反应,合成了一系列新型的噻唑衍生物。通过IR,1 H NMR,EIMS光谱数据和元素分析证实了新合成的化合物的结构。最初,通过确定化合物的LD(50)来测定化合物的急性毒性。筛选所有化合物的抗心律失常和抗凝活性,与普鲁卡因酰胺和利多卡因作为阳性对照相比,它们显示出较高的抗心律失常活性。报道了合成化合物的详细合成,光谱数据,LD(50)和药理活性。

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