We describe here the synthesis of a library of thirty-eight squaric derivatives and the evaluation of activity against papain-, falcipain-2- and a chloroquine-resistant strain of P. falciparum. The most active compounds combine significant antiplasmodial activity with minimal cytotoxicity.
Abstract—A new efficient method for deprotection of TBDMS derivatives of phenols, primary alcohols, carboxylic acids and secondary amines, consisting of SbCl5 and MeCN with 0.1% water (w/v), is reported. It effects inter alia desilylation of a CH2OTBDMS group in the presence of a ketal function.
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