Synthesis and biological evaluation of some 6-substituted purines

We report herein the synthesis and the in vitro antileishmanial evaluation of a series of 6-substituted purines. The most active compounds against Leishmania amazonensis promastigotes were 6-(3′-chloropropylthio)purine 2 (D.A. Benson, I. Karsch-Mizrachi, D.J. Lipman, J. Ostell, B.A. Rapp, D.L. Wheeler, Genbank. Nucleic Acids Res. 28 (2000) 15–18; E.V. Aleksandrova, P.M.I.E. Valashek, J. Med. Pharm. Chem. 35 (2001) 172–173), 6-(3′-(thioethylamine)propylthio)purine 5, 6-(α-aceticacidthio)purine 7 and 6-(6′-deoxy-1′-O-methyl-β-d-ribofuranose)purine 14 with an IC50 = 50, 50, 39 and 29 μM, respectively.

We report herein the synthesis and the in vitro antileishmanial evaluation of a series of 6-substituted purines. The most active compounds against Leishmania amazonensis were 6-(3′-chloropropylthio)purine, 6-(3′-(thioethylamine)propylthio)purine, 6-(α-aceticacidthio)purine and 6-(6′-deoxy-1′-O-methyl-β-d-ribofuranose)purine.Figure optionsDownload as PowerPoint slide