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

ISSN: 1875-6638 (Online)
ISSN: 1573-4064 (Print)


Volume 11, 8 Issues, 2015


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Medicinal Chemistry

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


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

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

Affiliation: College of Life Science and Bioengineering, Beijing University of Technology, Beijing 100124, China.

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.




Keywords:

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



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Article Details

Volume: 11
Issue Number: 2
First Page: 180
Last Page: 187
Page Count: 8
DOI: 10.2174/1573406410666140829154131
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