N-芳甲酰基-N′-取代嘧啶基硫脲类化合物的合成与初步活性研究

Synthesis and activity study of N-(substituted)benzoyl-N′-substituted pyrimidinyl thiourea derivatives

目的合成N-芳甲酰基-N′-取代嘧啶基硫脲类化合物,并初步测试其对血管平滑肌细胞增殖的抑制活性。方法以2-氨基-5-溴-4-取代嘧啶与芳甲酰基异硫氰酸酯反应,得到一系列N-芳甲酰基-N′-取代嘧啶基硫脲类化合物;采用MTT法测定目标化合物对血清诱导的血管平滑肌细胞增殖的抑制活性。结果与结论合成的10个目标化合物,均未见文献报道,所有目标化合物结构经1H-NMR及MS确证;活性测试结果表明,化合物6b、6 c、6 g、6 j具有一定的血管平滑肌细胞增殖抑制活性。

Aim To synthesize a new series of N-（substituted）benzoyl-N′-substituted pyrimidinyl thiourea derivatives and to evaluate their inhibitory activities against vascular smooth muscle cells proliferation.Methods The subject compounds could be obtained by direct amination of（substituted）benzoyl isothiocyanate with 2-amino-5-bromo-4-substituted pyrimidine derivatives.The inhibitory effect of the target compounds on VSMC proliferation was investigated by MTT.Results and conclusion Ten target new compounds were first synthesized and verified by 1H-NMR and MS.Compound 6b,6c,6g and 6j exhibited moderate inhibitory activities against vascular smooth muscle cells proliferation.