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

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1HNMR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100μmol·L-1,有待对此类化合物作进一步细胞水平的活性评价。

A series of novel quinolinone acid-containing compounds were designed and synthesized.Their structures were confirmed with 1 H 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 IC 50 100 μmol·L^-1.