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

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

Volume: 11 Issue: 2

Author(s): Liming Hu, Zhipeng Li, Zhanyang Wang, Gengxin Liu, Xianzhuo He, Xiaoli Wang and Chengchu Zeng

Affiliation:

Keywords: Aromatic diketones, desmosdumotin D, HIV IN inhibitory activity, integrase inhibitor, molecular docking.

Abstract: 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.

Cite this article as:

Hu Liming, Li Zhipeng, Wang Zhanyang, Liu Gengxin, He Xianzhuo, Wang Xiaoli and Zeng Chengchu, Design, Synthesis and Biological Activity of Aromatic Diketone Derivatives as HIV-1 Integrase Inhibitors, Medicinal Chemistry 2015; 11 (2) . https://dx.doi.org/10.2174/1573406410666140829154131