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Synthesis of and HIV-1 Integrase Inhibition by 2-[7-(Fluorobenzyloxy)-4-Oxo-4hchromen-3-Yl]-1-Hydroxyimidazoles

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A series of six new 2-[7-(fluorobenzyloxy)-4-oxo-4H-chromen-3-yl]-1-hydroxyimidazoles were synthesized and characterized as potential HIV-1 integrase inhibitors. Prototropic tautomerism of the obtained 1-hydroxyimidazoles was discussed. Their ability to inhibit integrase catalytic activity in 3′-terminal processing and chain transfer reactions was studied. It was shown that these compounds did not exhibit noticeable inhibition.

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Acknowledgments

The biological studies (determination of the inhibitory activities of the compounds) were sponsored by RSF Grant No. 14-14-00489.

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Authors and Affiliations

  1. D. I. Mendeleev University of Chemical Technology of Russia, 9 Miusskaya Sq, Moscow, 125047, Russia

    P. A. Nikitina, I. I. Tkach & V. P. Perevalov

  2. Department of Chemistry and A. N. Belozersky Institute of Physical and Chemical Biology, Lomonosov Moscow State University, Moscow, 119991, Russia

    E. S. Knyazhanskaya & M. B. Gottikh

Authors
  1. P. A. Nikitina
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  2. I. I. Tkach
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  3. E. S. Knyazhanskaya
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  4. M. B. Gottikh
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  5. V. P. Perevalov
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Corresponding author

Correspondence to P. A. Nikitina.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 50, No. 8, pp. 16 – 21, August, 2016.

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Nikitina, P.A., Tkach, I.I., Knyazhanskaya, E.S. et al. Synthesis of and HIV-1 Integrase Inhibition by 2-[7-(Fluorobenzyloxy)-4-Oxo-4hchromen-3-Yl]-1-Hydroxyimidazoles. Pharm Chem J 50, 513–518 (2016). https://doi.org/10.1007/s11094-016-1479-x

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  • DOI: https://doi.org/10.1007/s11094-016-1479-x

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