Amr Abd El-Galil E, Sabrry Nermien M, Abdalla Mohamed M, Abdel-Wahab Bakr F
Applied Organic Chemistry Department, National Research Center, El-Tahrir Street, Dokki, Cairo, Egypt.
Eur J Med Chem. 2009 Feb;44(2):725-35. doi: 10.1016/j.ejmech.2008.05.004. Epub 2008 May 15.
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.
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,合成了一系列新型噻唑衍生物。通过红外光谱(IR)、核磁共振氢谱(¹H NMR)、电子轰击质谱(EIMS)光谱数据和元素分析确定了新合成化合物的结构。首先,通过测定化合物的半数致死量(LD₅₀)来检测其急性毒性。对所有化合物进行抗心律失常和抗凝活性筛选,与作为阳性对照的普鲁卡因酰胺和利多卡因相比,它们显示出高抗心律失常活性。报道了合成化合物的详细合成方法、光谱数据、LD₅₀和药理活性。