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2004
Pyrimidine derivatives
R 0510
Synthesis and anti-HIV-1 Activity of 2-[2-(3,5-Dimethylphenoxy)ethylthio]py— Alkylation of 2-thiouracils (I) with bromoethoxyxylene (II)
48- 130 rimidin-4(3H)-ones.
takes place exclusively at the sulfur atom to furnish the title compounds (III) (10 examples) in moderate to good yields. The obtained 6- benzyl derivatives (IIIb) and (IIIc)
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. — (NOVIKOV, M. S.; OZEROV, A. A.; SIM, O. G.;
BUCKHEIT, R. W.; Chem. Heterocycl. Compd. (N. Y.) 40 (2004) 1, 37-42; Sci.-Res.
Inst. Pharmacol., Volgograd Med. Acad., Volgograd 400066, Russia; Eng.) —
H. Toeppel
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