Structurally diverse 5-substituted pyrimidine nucleosides as inhibitors of Leishmania donovani promastigotes in vitro

The following structurally diverse 5-substituted-2′-deoxyuridine nucleosides displayed potent in vitro antileishmanial activity: 5-formyl, 5-(2,2,-dicyanovinyl)-, 5-(2-cyano-2-ethoxycarbonylvinyl), 5-(2-cyano-2-methoxycarbonylvinyl)-, 5-(2-amino-3-cyano-5-oxo-5,6,7,8-tetrahydro-4H-chromen-4-yl)- and related congeners, and the 5-(3-methyl-5-oxo-1-phenyl-4,5-dihydro-4H-pyrazol-4-ylidene) group.

Graphical abstractA series of 5-substituted pyrimidine nucleosides with R substituents ranging from formyl, to dicyanovinyl, to substituted chromenes, and including a pyrazolone, were all potent inhibitors of Leishmania donovani promastigotes.Figure optionsDownload full-size imageDownload as PowerPoint slide