Synthesis and in vitro antileishmanial activity of 5-substituted-2'-deoxyuridine derivatives |
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Authors: | Peyron Corinne Benhida Rachid Bories Christian Loiseau Philippe M |
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Affiliation: | Laboratoire de Chimie Bioorganique UMR-CNRS 6001, Université de Nice-Sophia Antipolis, Parc Valrose F-06108, Nice Cédex 2, France. |
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Abstract: | We report herein the synthesis and the in vitro antileishmanial evaluation of 5-substituted-2'-deoxyuridine nucleosides. The most active compound against Leishmania donovani promastigotes was Thia-dU (3a) with an IC50 =3 microM. This compound exhibited the same activity as zidovudine (3'-azido-2'-deoxythymidine) used as nucleoside reference compound. Considering the cytotoxicity of synthetic compounds on peritoneal murine macrophages, the most toxic compound was MeThio-dU (3d) with a MTC at 10 microM. Only Methia-dU (3b) was active against intramacrophagic amastigotes with an IC50 =6.5 microM. This latter can now be evaluated in vivo, for further investigations through structure-based drug design. |
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Keywords: | Nucleosides Antileishmanial activity |
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