1. Academic Validation
  2. Parallel synthesis and anti-malarial activity of a sulfonamide library

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

Affiliation

  • 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.
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.

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