Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors

作者：Hu Liming^*; Li Zhipeng; Wang Zhanyang; Liu Gengxin; He Xianzhuo; Wang Xiaoli; Zeng Chengchu

来源：Medicinal Chemistry, 2015, 11(2): 180-187.

DOI：10.2174/1573406410666140829154131

• Aromatic diketones
• desmosdumotin D
• HIV IN inhibitory activity
• integrase inhibitor
• molecular docking

A series of aromatic diketone derivatives were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated to determine their ability to inhibit the strand transfer process of HIV-1 integrase. The results indicate that (Z)-1-(3-acetyl-2-hydroxy-4,6-dimethoxyphenyl)-3-hydroxy-3-(substituted) phenylprop-2-en-1-one (5a-5d) can moderately inhibit HIV-1 integrase. The cyclization and condensation products (6a-6c and 7e-7f) of compounds 5a-5d show poor inhibitory activity against HIV-1 integrase. The molecular docking results indicate that the different types of compounds act on HIV-1 integrase in different ways, and these results can explain the differences in the inhibitory activities.

• 出版日期2015
• 单位北京工业大学