喹啉酮酸类化合物的设计合成与抗HIV-1整合酶活性研究

Design, synthesis of quinolinone acid-containing compounds with anti-HIV integrase activity

摘要:
以HIV-1整合酶为靶点, 设计并合成了8个含喹啉酮酸类新化合物, 其结构经¹H NMR和MS确证。用酶联免疫吸附剂测定法 (ELISA方法) 测定了其体外抗HIV-1整合酶活性。结果表明, 目标化合物中 D-2、D-4和D-7对HIV-1整合酶的抑制活性小于100 µmol·L⁻¹, 有待对此类化合物作进一步细胞水平的活性评价。

Abstract:
A series of novel quinolinone acid-containing compounds were designed and synthesized. Their structures were confirmed with ¹H NMR and MS. The target compounds were tested for anti-HIV-1 integrase activities in vitro with enzyme linked immunosorbent assay (ELISA). The result showed that D-2, D-4 and D-7 have anti-integrase activity with IC₅₀< 100 µmol·L⁻¹.