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目的设计合成新型喹啉酮类化合物并研究其对HIV-1逆转录酶的抑制活性。方法以丙二酸二乙酯为原料,经烷基化反应得2-取代丙二酸二乙酯,它再与对氯苯胺或3,4-二氟苯胺缩合,用多聚磷酸环合,最后与卤代烃、取代苯甲酰氯反应得到目标化合物;并对目标化合物进行了初步的体外HIV-1逆转录酶抑制活性筛选。结果与结论合成了24个新化合物,其结构经IR、1H-NMR、MS谱及元素分析确证。初步的药理试验表明,24个目标化合物中有6个化合物具有一定的HIV-1逆转录酶抑制活性。
Aim To design and synthesize novel quinolinones and study their inhibitory activity against HIV-1 reverse transcriptase. Methods Diethyl malonate was used as raw material to obtain 2-substituted diethyl malonate by alkylation. It was then condensed with p-chloroaniline or 3,4-difluoroaniline, cyclized with polyphosphoric acid, Finally, the target compound was obtained by reaction of halogenated hydrocarbon and substituted benzoyl chloride. The target compound was preliminarily screened for HIV-1 reverse transcriptase inhibitory activity. RESULTS AND CONCLUSIONS 24 new compounds were synthesized and their structures were confirmed by IR, 1H-NMR, MS and elemental analysis. Preliminary pharmacological tests showed that 6 out of 24 target compounds had some HIV-1 reverse transcriptase inhibitory activity.