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2004-05-06 - Article/Dans un journal avec peer-review - Anglais - 6 page(s)

Mayence A., Vanden Eynde Jean-Jacques , Krogstad D.J., Krogstad F.M., Cushion M.T., Huang T.L., "Parallel Solution-phase Synthesis of Conformationally Restricted Congeners of Pentamidine and Evaluation of their Antimalarial Activity" in Journal of Medicinal Chemistry, 47, 10, 2700 - 2705

  • Edition : American Chemical Society, Washington (DC)
  • Codes CREF : Chimie organique (DI1313)
  • Unités de recherche UMONS : Chimie organique (S836)
Texte intégral :

Abstract(s) :

(Anglais) Conformationally restricted bisbenzamidines and related congeners have been synthesized and evaluated for activity against two Plasmodium falciparum strains. The most active compounds, bisbenzamidines linked by a 1,4-piperazinediyl core, had IC(50) values between 3 and 18 nM against both chloroquine-susceptible and -resistant parasites and IC(50) values for cytotoxicity greater than 5 microM, using the A549 human lung epithelial cell line. DNA binding affinity, as estimated by DeltaT(m), did not correlate with either antiparasite effects or cytotoxicity. Each of the active bisbenzamidines interfered with the formation of hemozoin in cell-free systems.

Identifiants :
  • PMID : 15115412
  • DOI : 10.1021/jm030545e