Parallel Synthesis and Anti-Malarial Activity of a Sulfonamide Library

Bioorganic & Medicinal Chemistry Letters
2002.0

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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