Parallel synthesis and anti-malarial activity of a sulfonamide library

  • Bioorg Med Chem Lett. 2002 Sep 16;12(18):2595-8. doi: 10.1016/s0960-894x(02)00475-4.
A Ryckebusch  1 ,  R Déprez-Poulain ,  M A Debreu-Fontaine ,  R Vandaele ,  E Mouray ,  P Grellier ,  C Sergheraert
Affiliations
  • 1. Institut de Biologie et Institut Pasteur de Lille, UMR CNRS 8525, Université de Lille II, 1 rue du Professeur Calmette, B.P. 447, 59021, Lille, France.
PMID: 12182868 DOI: 10.1016/s0960-894x(02)00475-4
Abstract

Solution-phase synthesis and evaluation of a library of 31 sulfonamides as inhibitors of a chloroquine-resistant strain of Plasmodium falciparum are described. The most potent compound displayed an activity 100-fold better than chloroquine. Experiments using a fluorescent sulfonamide derivative suggest that their site of action inside the Parasite is different to that of chloroquine.