A trio of quinoline-isoniazid-phthalimide with promising antiplasmodial potential: Synthesis, in-vitro evaluation and heme-polymerization inhibition studies

Quinoline-isoniazid-phthalimide triads have been synthesised to assess their antiplasmodial efficacy and cytotoxicity against chloroquine-resistant W2 strain of P. falciparum and Vero cells, respectively. Most of the synthesized compounds displayed IC50 in lower nM range and appeared to be approximately five to twelve fold more active than chloroquine. Heme-binding studies were also carried out to delineate the mode of action. The promising compounds with IC50s in range of 11-30 nM and selectivity index >2800, may act as promising template for the design of new antiplasmodials.

Automated summary

Quinoline-isoniazid-phthalimide triads synthesized for evaluating antiplasmodial efficacy against chloroquine-resistant P. falciparum and cytotoxicity on Vero cells showed promising results with some compounds having IC50 in the range of 11-30 nM and high selectivity index, indicating their potential as templates for new antiplasmodial drugs.