Synthesis and anti- Plasmodium falciparum evaluation of novel pyrazolopyrimidine derivatives

AbstractNine 1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives with different substituents in the 4-position of the phenyl group and benzenesulfonamide moiety were synthesized and evaluated againstPlasmodium falciparum. Six compounds exhibited activity in vitro against the chloroquine-resistant clone W2 with IC50 values ranging from 5.13 to 12.22  µM. The most active derivative with substituents R1 = F / R2 = CH3 exhibited an IC50 value of 5.13  µM and an IS value of 62.90, which was higher than that of the control drug sulfadoxine. For this reason, it is possible to conclude that the 1H-pyrazolo[3,4-d]pyrimidine system is promising as a prototype for further studies of antimalarial candidates.

Source: Medicinal Chemistry Research - June 20, 2018 Category: Chemistry Source Type: research