Pyrazolyl amide-chalcones conjugates: Synthesis and antikinetoplastid activity.

Autor: Agarwal DS; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, 2520, South Africa., Beteck RM; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, 2520, South Africa., Mabille D; Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium., Caljon G; Laboratory of Microbiology, Parasitology and Hygiene, Infla-Med Centre of Excellence, University of Antwerp, Antwerp, Belgium., Legoabe LJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, 2520, South Africa. lesetja.legoabe@nwu.ac.za.
Jazyk: angličtina
Zdroj: Naunyn-Schmiedeberg's archives of pharmacology [Naunyn Schmiedebergs Arch Pharmacol] 2024 Oct 21. Date of Electronic Publication: 2024 Oct 21.
DOI: 10.1007/s00210-024-03524-7
Abstrakt: 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.
(© 2024. The Author(s).)
Databáze: MEDLINE
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