Synthesis and in vitro antileishmanial activity of 5-substituted-2'-deoxyuridine derivatives.

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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Peyron C,Benhida R,Bories C,Loiseau PM

doi

10.1016/j.bioorg.2005.07.001

subject

Has Abstract

pub_date

2005-12-01 00:00:00

pages

439-47

issue

6

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(05)00074-X

journal_volume

33

pub_type

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