| Summary: | In order to prepare, at low cost, new compounds active against <i>Plasmodium falciparum</i>, and with a less side-effects, we have designed and synthesized a library of 1,4-disubstituted piperidine derivatives from 4-aminopiperidine derivatives <b>6</b>. The resulting compound library has been evaluated against chloroquine-sensitive (3D7) and chloroquine-resistant (W2) strains of <i>P. falciparum.</i> The most active molecules—compounds <b>12d</b> (13.64 nM (3D7)), <b>13b</b> (4.19 nM (3D7) and 13.30 nM (W2)), and <b>12a</b> (11.6 nM (W2))—were comparable to chloroquine (22.38 nM (3D7) and 134.12 nM (W2)).
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