{Reference Type}: Journal Article
{Title}: New series of monoamidoxime derivatives displaying versatile antiparasitic activity.
{Author}: Tabélé C;Cohen A;Curti C;Bouhlel A;Hutter S;Remusat V;Primas N;Terme T;Azas N;Vanelle P;
{Journal}: Eur J Med Chem
{Volume}: 87
{Issue}: 0
{Year}: Nov 2014 24
{Factor}: 7.088
{DOI}: 10.1016/j.ejmech.2014.07.113
{Abstract}: Following the promising antileishmanial results previously obtained in monoamidoxime series, a new series of derivatives was synthesized using manganese(III) acetate, Wittig reactions and Suzuki-Miyaura cross coupling reactions. Pharmacomodulation in R(1), R(2) or R(3) substituents on the amidoxime structure is shown to influence antiprotozoan activity in vitro: a monosubstituted phenyl group in R1 (32-35) led to an activity against Leishmania donovani promastigotes (32, IC50 = 9.16 μM), whereas a polysubstituted group (36-37) led to an activity against Plasmodium falciparum (36, IC50 = 2.76 μM). Modulating chemical substituents in R(2) and R(3) only influenced the antiplasmodial activity in vitro. This suggests that the amidoxime scaffold has properties that could make it a promising new antiparasitic pharmacophore.