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To expand the structural diversity of Matijin-Su (MTS) derivatives and explore novel anti-HBV activity compounds, a series of fluorinated dipeptidomimetics of MTS were designed and synthesized by using trifluoromethyl substituted methylamine unit as bioisostere to replace the amide bond of the MTS derivatives. The structures of all target compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, HRMS, or ESI-MS, and the crystal structure of 10' was determined by X-ray single crystal diffraction. Their inhibitory activity against hepatitis B virus (HBV) in vitro were evaluated using HepG2 2.2.15 cell model. The results showed that all target compounds had inhibitory effect on HBV DNA replication, the IC50 of 14e, 14f, and 14k were 0.37, 0.29, and 0.79 μmol·L-1, respectively.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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