Parallel synthesis and anti-malarial activity of a sulfonamide library.
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.
Ryckebusch
A
A
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.
Déprez-Poulain
R
R
Debreu-Fontaine
M A
MA
Vandaele
R
R
Mouray
E
E
Grellier
P
P
Sergheraert
C
C
D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D006801:Humans; D008856:Microscopy, Fluorescence; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D013449:Sulfonamides