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以马蹄金素[N-(N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇,MTS]为先导化合物,设计并合成了11个NO供体型马蹄金素衍生物,所有目标产物均未见文献报道,其结构经NMR,ESI-MS确认.以HepG2 2.2.15细胞为乙肝病毒载体,对合成的马蹄金素衍生物进行了抗乙肝病毒活性测试.结果表明,在测试浓度范围内,化合物6d,6e,6g具有抗HBV活性,其半数抑制浓度分别为6.88,37.51,11.07μmol/L.其中,化合物6d和6g的半数抑制浓度优于MTS(11.16μmol/L),且具有较高的抑制率,具有进一步研究开发的价值.
In this study, 11 NO donor horseshoe were designed and synthesized with the use of hoofensin [N- (N-benzoyl-L-phenylalanyl) -O-acetyl-L-phenylalaninol, MTS] All the target products were not reported in the literature, and their structures were confirmed by NMR and ESI-MS. The HepG2 2.2.15 cells were tested for their anti-HBV activity against hepatitis B virus The results showed that compounds 6d, 6e and 6g had anti-HBV activity in the range of concentration tested, and their half-maximal inhibitory concentrations were 6.88, 37.51 and 11.07 μmol / L, respectively, and the half- 11.16μmol / L), and has a higher inhibition rate, with further research and development value.