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Synthesis 2007(13): 1955-1960  
DOI: 10.1055/s-2007-983732
PAPER
© Georg Thieme Verlag Stuttgart · New York

Novel Synthesis and Anti-HIV-1 Activity of 2-Arylthio-6-benzyl-2,3-dihydro-1H-pyrimidin-4-ones (Aryl S-DABOs)

Youssef L. Alya, Erik B. Pedersen*a, Paolo La Collab, Roberta Loddob
a Nucleic Acid Center, Department of Physics and Chemistry, University of Southern Denmark, Campusvej 55, 5230 Odense M, Denmark
Fax: +4566158780; e-Mail: ebp@ifk.sdu.dk ;
b Dipartimento di Scienze e Tecnologie Biomediche, Sezione di Microbiologia e Virologia Generale e Biotecnologie Microbiche, Universitá di Cagliari, Cittadella Universitaria, 09042 Monserrato, Italy
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Publication History

Received 22 December 2006
Publication Date:
18 June 2007 (online)

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Abstract

The synthesis and the anti-HIV-1 activity of a series of 2-arylthio-6-benzyl-2,3-dihydro-1H-pyrimidin-4-ones (aryl S-DABOs) are reported. These compounds were synthesized via a coupling reaction of the corresponding 6-benzyl-2-thiouracils with aryl iodides in the presence of neocuproine hydrate, copper(I) iodide, and sodium tert-butoxide. Target compounds showed moderate activity against HIV-1.

Key words

medicinal chemistry - antiviral agents - HIV - non-nucleosides - S-DABO

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1

On leave from Chemistry Department, Faculty of Education Kafr El-Sheikh branch, Tanta University, Kafr El-Sheikh, Egypt.

2

A research center funded by the Danish National Research Foundation for Studies on Nucleic Acid Chemical Biology.

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