Synthesis and Anti-HIV-1 Activity of 2-[2-(3,5-Dimethylphenoxy)ethylthio]pyrimidin-4(3H)-ones |
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Authors: | M S Novikov A A Ozerov O G Sim R W Buckheit |
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Institution: | (1) Scientific-Research Institute of Pharmacology, Volgograd Medical University, Volgograd, 400131, Russia;(2) TherImmune Research Corp., Maryland, USA |
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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 mM respectively. |
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Keywords: | 2-[2-(3 5-dimethylphenoxy)ethylthio]pyrimidin-4(3H)-ones S-alkylation anti-HIV-1 activity |
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