Synthesis and Evaluation of Substituted Pyrazoles: Potential Antimalarials Targeting the Enoyl‐ACP Reductase of Plasmodium Falciparum
Sanjay Kumar, Gyanendra Kumar, Mili Kapoor, Avadhesha Surolia, Namita Surolia · Synthetic Communications · 2006
A series of 1,5‐ and 1,3‐diarylsubstituted pyrazoles were designed, synthesized, and evaluated for their ability to inhibit enoyl‐ACP reductase of Plasmodium falciparum. The inhibitory activity of these synthesized compounds was evaluated in a continuous spectrophotometric assay. Of all the compounds analyzed, NAS‐81 and NAS‐39 inhibited the enzyme with IC50 values of 30 µM and 50 µM, respectively. The mode of ligand binding was investigated by docking the synthetic inhibitors at the active site of the crystal structure of the enzyme.