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

Détermination structurale de triterpenoïdes isolés des feuilles de Combretum glutinosium Perr. Ex DC (Combretaceae)

In the structure of the title compound, C₁₇H₁₈N₂O₇·H₂O, hydrogen bonds link three molecules to the water molecule. Additional hydrogen-bonding interactions connect two molecules via the amide nitrogen donor and two methoxy oxygen acceptors. This three-dimensional hydrogen-bond network has no particular directionality, and a slight disorder of two methoxy groups is observed. According to force-field calculations, weaker but more extended van der Waals interactions show a larger stabilization effect than the hydrogen-bond interactions, while hydrogen-bond analysis suggests that polymorphs of the compound may be found in the future.