Volume 31, Issue 51
Heterocyclic Compounds
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ChemInform Abstract: Synthesis of Anellated Analogues of 6-Benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442) Using 1,3-Oxazine-2,4(3H)-diones as Key Intermediates.

Janus S. Larsen

Janus S. Larsen

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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Lene Christensen

Lene Christensen

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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Gitte Ludvig

Gitte Ludvig

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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Per T. Joergensen

Per T. Joergensen

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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Erik B. Pedersen

Erik B. Pedersen

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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Claus Nielsen

Claus Nielsen

Dep. Chem., Odense Univ., DK-5230 Odense, Den.

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First published: 31 May 2010

Abstract

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ChemInform Abstract

Two new MKC-442 analogues (X) and (XII) with fixed orientation of the phenyl group in the molecule are synthesized and their biological activity is investigated. Key intermediates of the synthesis are the oxazine diones (III) which are obtained via two new strategies. All new compounds are tested for their activity against HIV-1 in MT-4 cells. However, only the compounds (X) and (XII) show activity against HIV-1, but at considerably higher concentrations than the reference compound MKC-442.

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