【作者】 唐胜； 李玉环； 高丽梅； 蒋建东； 宋丹青；

【Author】 Sheng Tang,Yu-Huan Li,Li-Mei Gao,Jian-Dong Jiang,Dan-QingSong (Institute of Medicinal Biotechnology,Chinese Academy of Medical Science & Peking Union Medical College,Beijing 100050,China)

【机构】 中国医学科学院北京协和医学院医药生物技术研究所；

【摘要】 目的:设计、合成全新结构的抗柯萨奇病毒的槐果酸衍生物。方法 :以槐果碱为原料,通过水解开环,保护、取代、脱保护等不同的反应,共设计合成22个化合物,结构经核磁共振氢谱、质谱等确证。体外测定其抗柯萨奇病毒B3(CVB3)活性,并对活性好的化合物进行了抗柯萨奇病毒B6(CVB6)、A16(CVA16)活性研究。结果 :优选出化合物13h,其抗柯萨奇病毒B3活性为1.08μM,选择性治疗指数为106.9,同时对柯萨奇病毒B6和A16也有一定活性,为全新结构的抗柯萨奇病毒的候选物。结论 :化合物13h作为抗柯萨奇候选物,值得进一步研究。更多还原

【Abstract】 object:To design,synthesize and select novel N-substituted sophocarpinic acid derivatives against Coxsackievirus.method:22 compounds were synthesized from sophocarpine by reactions with Hydrolysis,open loop,adding protection group,substitution,off protecting group.Whose structures were confirmed by the methods of 1 H-NMR and MS.The activity against Coxsackievirus B3 (CVB3) was tested in vivo,and the activities of Coxsackievirus B6(CVB6) and A16(CVA16) were also tested for the compounds with good activity of anti-coxsackievirus B3.result:The novel compound 13h (IC50=1.08μM,IS=106.9),which has some activities of Coxsackievirus B6(CVB6) and A16(CVA16),was selected as a candidate against Coxsackievirus.conclusion:The compound 13h as a candidate against Coxsackievirus is worthy further study.更多还原