Cheng Xin-yue, Tang Sheng, Kong Lan-ying, Li Yu-huan, Song Dan-qing
Yao Xue Xue Bao. 2016 Apr;51(4):606-12.
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. Structure- activity 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 IC(50) 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.
12 - N - m - 氰基苯磺酰基苦参丁基甲基醚是一种具有新型结构骨架的强效抗柯萨奇病毒B3（CVB3）药物。以该化合物为先导，共合成了15种新型目标化合物，并采用细胞病变效应（CPE）法评估了它们的抗CVB3活性。构效关系（SAR）表明，11 - 侧链长度缩短不利于保持良好的抗病毒活性。在新合成的化合物中，化合物c1表现出良好的抗CVB3活性，IC(50)为7.1 μmol·L(-1)，选择性指数（SI）为35.5，与先导化合物相似。SAR结果为进一步优化这些化合物的分子结构提供了有用信息。
