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Nucleic Acids Symposium Series 2004 48(1):3-4; doi:10.1093/nass/48.1.3
© 2004 by Oxford University Press
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Synthesis and antiviral activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil against HIV-1

Tokumi Maruyama1,2, Shigetada Kozai2, Yosuke Demizu1, Myriam Witvrouw3, Christophe Pannecouque3, Jan Balzarini3, Robert Snoeck3, Graciella Andrei3 and Erik De Clercq3

1 Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, Shido, Sanuki City, Kagawa 769-2193, Japan, 2 Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Yamashiro-cho 180, Tokushima 770-8514, Japan, 3 Rega Instituut, Katholieke, Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium

1,3-Disubstituted uracils were obtained from uracil by the stepwise alkylation at N-1 and N-3 position with alkyl halide/alkali or alcohol under Mitsunobu conditions. The antiviral activity against HIV-1 of these compounds was examined to find that 1-cyanomethyl-3-(3,5-dimethylbenzyl)uracil and 1-phenyl-3-(3,5-dimethyl-benzyl)uracil showed powerful inhibition.


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