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目的设计合成7-苯甲酰基中氮茚-1-羧酸乙酯类化合物,并对其抗HIV-1活性进行初步研究。方法以异烟酸、溴乙酸苄酯、丙炔酸乙酯为原料,经取代、Friedel-Crafts反应、1,3-偶极环加成反应、水解、缩合得到目标化合物;采用荧光筛选方法对目标化合物抗HIV-1病毒感染因子(viral infectivity factor,VIF)活性进行评价。结果共合成30个未经文献报道的新化合物,其结构经1H-NMR、13C-NMR、HRMS确证;活性结果表明,化合物30、31、36、37等4个化合物抗HIV-1活性与先导化合物相当。结论 7-苯甲酰基中氮茚-1-羧酸乙酯类化合物作为HIV-1 VIF复合物抑制剂,中氮茚环与取代芳环之间含3～4个原子长度为保持活性所必须,进一步的构效关系值得继续研究。
OBJECTIVE To design and synthesize ethyl 7-benzoylindolizine-1-carboxylate and study its anti-HIV-1 activity. Methods The target compounds were synthesized from isonicotinic acid, benzyl bromoacetate and ethyl propiolate via Friedel-Crafts reaction, 1,3-dipolar cycloaddition, hydrolysis and condensation. The target compound is evaluated against HIV-1 viral infectivity factor (VIF) activity. Results A total of 30 new compounds were synthesized and their structures were confirmed by 1H-NMR, 13C-NMR and HRMS. The results showed that the compounds 30, 31, 36, 37 and other 4 compounds had anti-HIV-1 activity and lead The compound is equivalent. Conclusion 7-benzoylindolizine-1-carboxylic acid ethyl ester compounds as HIV-1 VIF complex inhibitors, indol ring and substituted aromatic ring containing 3 to 4 atoms in length necessary to maintain activity , Further structure-activity relationship worth to continue to study.