Journal Article
Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity
Devesh S. Agarwal; Richard M. Beteck; Dorien Mabille; Guy Caljon; Lesetja J. Legoabe
Naunyn-Schmiedeberg's Archives of Pharmacology · Vol. 398, Issue 4 · pp. 4199-4210 · 2025
Abstract
A series of novel pyrazolyl amide-chalcones conjugates was synthesized in five steps and evaluated against a range of medically important kinetoplastid parasites including Trypanosoma cruzi , Trypanosoma brucei brucei , Trypanosoma brucei rhodesiense and Leishmania infantum . In addition, the series was also tested for in vitro cytotoxicity activity against human lung fibroblasts and primary mouse macrophages. Among all synthetised compounds, 9b was found to be the most active against T. b. brucei with an IC 50 value of 0.51 ± 0.06 μM. Against T. b. rhodesiense , 9n was found to be the most potent with an IC 50 value of 0.46 ± 0.07 μM. While against L. infantum , 9a was found to be most active with an IC 50 value of 7.16 ± 1.88 μM. Based on the results and SAR, further modifications will be carried out to increase potency. Graphical Abstract