Synthesis and Anti-HBV Activity Evaluation of Matijin-Su Derivatives Containing Trifluoromethyl / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 1045-1053, 2019.
Article
in Chinese
| WPRIM
| ID: wpr-857969
ABSTRACT
OBJECTIVE:
To design and synthesize derivatives of Matijin-Su (MTS) containing trifluoromethyl group and investigate their anti-HBV activities in vitro.METHODS:
Taking MTS as lead compound, target compounds were prepared by acylation, alkylation and hydrolysis, etc. The cytotoxicities and anti-HBV activities of the target compounds were tested with MTT method.RESULTS Twenty derivatives of MTS containing trifluoromethyl were synthesized and their structures were confirmed by 1H-NMR, 13C-NMR and MS(ESI). The anti-HBV activities of those compounds were evaluated in HepG2 2.2.15 cells. The screeningRESULTS:
showed that compounds 3b, 6a, 6c, 6d, 6h-6j and 6n had HBV inhibitory effect for HepG2 2.2.15 cells. Compounds 3b, 6d and 6n exhibited significant anti-HBV activity with IC50 values of 11.74, 8.73 and 11.41 μmol•L-1.CONCLUSION:
Incorporation of trifluoromethyl into MTS derivatives can lead to profound changes in their anti-HBV activity, and could be worth of further research.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Chinese Pharmaceutical Journal
Year:
2019
Type:
Article
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