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Pharmaceutical Chemistry Journal

, Volume 50, Issue 8, pp 513–518 | Cite as

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

  • P. A. Nikitina
  • I. I. Tkach
  • E. S. Knyazhanskaya
  • M. B. Gottikh
  • V. P. Perevalov
SEARCH FOR NEW DRUGS

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.

Keywords

1-hydroxyimidazoles prototropic tautomerism HIV-1 integrase inhibitors 

Notes

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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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  • P. A. Nikitina
    • 1
  • I. I. Tkach
    • 1
  • E. S. Knyazhanskaya
    • 2
  • M. B. Gottikh
    • 2
  • V. P. Perevalov
    • 1
  1. 1.D. I. Mendeleev University of Chemical Technology of RussiaMoscowRussia
  2. 2.Department of Chemistry and A. N. Belozersky Institute of Physical and Chemical BiologyLomonosov Moscow State UniversityMoscowRussia

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