Structure–activity relationship studies of antiplasmodial aminomethylthiazoles

Structure–activity relationship (SAR) studies around a previously reported antimalarial aminomethylthiazole pyrazole carboxamide 1 are reported. Several analogues were synthesised and profiled for in vitro antiplasmodial activity against the drug-sensitive Plasmodium falciparum malaria parasite strain, NF54. Although all the reported analogues exhibited inferior in vitro antiplasmodial activity (IC50 = 0.125–173 μM) relative to compound 1 (IC50 = 0.0203 μM), one analogue, compound 5a, retained submicromolar activity (IC50 = 0.125 μM).

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