3，4-二取代香豆素类衍生物的合成及其对HIV-1逆转录酶的抑制活性

基金项目: 中央高校基本科研业务费专项资金项目资助（No.JKQ2011005）

Synthesis and HIV-1 reverse transcriptase inhibitory activity of 3,4-disubstituted coumarin derivatives

摘要: 苯并六元杂环类化合物是重要的逆转录酶抑制剂，目前报道的活性较好的化合物在结构上都有一个疏水的苯环和与苯环相连的酰胺部分。通过对酰胺部分进行结构改造，探索其对HIV-1逆转录酶活性的影响。合成了一系列未见文献报道的3,4-二取代香豆素类化合物，其结构经IR，¹H NMR，MS及元素分析确证。初步的药理活性实验表明，23个化合物中有7个化合物具有一定的HIV-1逆转录酶抑制活性。
- 3,4-二取代香豆素 /
- HIV-1逆转录酶抑制剂 /
- 合成 /
- 抑制活性
Abstract: Benzo 6-membered heterocyclic compounds are important reverse transcriptase inhibitors.Active compounds reported in the literature have a hydrophobic benzene ring and an amide moiety connected with the benzene ring.Aiming at structural modification of amide part, a series of 3，4-disubstituted coumarin compounds were prepared.Their structures were confirmed by IR，MS，¹H NMR and element analysis.The results of the preliminary pharmacological test showed that seven out of twenty-three compounds possessed diverse HIV-1 reverse transcriptase inhibitory activity.
- 3,4-disubstituted coumarins /
- HIV-1 non-nucleoside reverse transcriptase inhibitors /
- synthesis /
- inhibitory activity