SYNTHESIS AND ANTI-HIV-1 ACTIVITY OF 2-[2-(3,5-DIMETHYLPHENOXY)ETHYLTHIO]PYRIMIDIN-4(3H)-ONES

Authors

  • М. С. Новиков Scientific-Research Institute of Pharmacology, Volgograd Medical University, Volgograd 400131
  • А. А. Озеров Scientific-Research Institute of Pharmacology, Volgograd Medical University, Volgograd 400131
  • О. Г. Сим Scientific-Research Institute of Pharmacology, Volgograd Medical University, Volgograd 400131
  • Р. У. Букхайт TherImmune Research Corp., Maryland

Keywords:

2-[2-(3,5-dimethylphenoxy)ethylthio]pyrimidin-4(3H)-ones, S-alkylation, anti-HIV-1 activity

Abstract

New 2-[2-(3,5-dimethylphenoxy)ethyl]thio derivatives of pyrimidin-4(3H)-one containing various substituents at positions 5 and 6 of the pyrimidine ring were synthesized. It was shown that alkylation of 2-thiouracils with 1-bromo-2-(3,5-dimethylphenoxy)ethane in DMF takes place exclusively at the sulfur atom. The obtained 6-benzyl and 6-(2,6-difluorobenzyl) derivatives have clearly defined virus-inhibiting properties with respect to type 1 human immunodeficiency virus in vitro and suppress its reproduction by 50% at concentrations of 1.3 and 11.2 µM respectively.

How to Cite
Novikov, M. S.; Ozerov, A. A.; Sim, O. G.; Buckheit, R. W. Chem. Heterocycl. Compd. 2004, 40, 37. [Khim. Geterotsikl. Soedin. 2004, 42.]

For this article in the English edition, see DOI 10.1023/B:COHC.0000023765.27571.40

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Published

2004-01-25

Issue

No. 1 (2004)

Section

Original Papers