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5-Formyl-2′-deoxyuridine-3′,5′-diacetate was converted to a small library of 5-substituted pyrimidine nucleoside N-acylamino acid amides by means of a Ugi multicomponent reaction. The reaction allowed introduction of various substituents at the acyl moiety, at the amino acid α-amide group, and at the amino acid carboxyl function. Evaluation of these novel 5-substituted nucleosides against vaccinia...
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 IC 50 =3μM. This compound exhibited the same activity as zidovudine (3′-azido-2′-deoxythymidine) used as nucleoside reference compound. Considering the cytotoxicity of synthetic compounds...
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