CHENG Xin-yue, TANG Sheng, KONG Lan-ying, LI Yu-huan, SONG Dan-qing. Synthesis and biological evaluation of 12-N-benzenesulfonyl matrinic ether derivatives as anti-coxsackievirus B3 agentsJ. Acta Pharmaceutica Sinica, 2016,51(4): 606-612. doi: 10.16438/j.0513-4870.2015-1011
Citation: CHENG Xin-yue, TANG Sheng, KONG Lan-ying, LI Yu-huan, SONG Dan-qing. Synthesis and biological evaluation of 12-N-benzenesulfonyl matrinic ether derivatives as anti-coxsackievirus B3 agentsJ. Acta Pharmaceutica Sinica, 2016,51(4): 606-612. doi: 10.16438/j.0513-4870.2015-1011

Synthesis and biological evaluation of 12-N-benzenesulfonyl matrinic ether derivatives as anti-coxsackievirus B3 agents

  • 12-N-m-Cyanobenzenesulfonyl matrinic butyl methyl ether is a potent anti-coxsackievirus B3(CVB3) agent bearing a novel structure skeleton. Taking this compound as a lead, totally 15 novel target compounds have been synthesized and evaluated for the anti-CVB3 activities using CPE method. Structureactivity relationship (SAR) demonstrated that the shorten-length of 11-side chain was not helpful for keeping the good anti-virus activity. Among the newly synthesized compounds, compound c1 displayed a good anti-CVB3 activity with the IC50 of 7.1 μmol·L-1 and SI of 35.5, similar to that of the lead. The SAR results provided useful information for further optimization of these compounds in the molecular structure.
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