| Autor: |
Bozdag M; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Mertens F; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Matheeussen A; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Van Pelt N; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Foubert K; Natural Products and Food Research and Analysis-Pharmaceutical Technology, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Hermans N; Natural Products and Food Research and Analysis-Pharmaceutical Technology, Department of Pharmaceutical Sciences, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., De Meyer GRY; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Augustyns K; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Martinet W; Laboratory of Physiopharmacology, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Caljon G; Laboratory of Microbiology, Parasitology and Hygiene, Department of Biomedical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium., Van der Veken P; Laboratory of Medicinal Chemistry, Department of Pharmaceutical Sciences, Infla-Med Centre of Excellence, University of Antwerp, Universiteitsplein 1, 2610 Wilrijk-Antwerp, Belgium. |
| Abstrakt: |
Herein, we report a series of 1,3-diarylpyrazoles that are analogues of compound 26 /HIT 8. We previously identified this molecule as a 'hit' during a high-throughput screening campaign for autophagy inducers. A variety of synthetic strategies were utilized to modify the 1,3-diarylpyrazole core at its 1-, 3-, and 4-position. Compounds were assessed in vitro to identify their cytotoxicity properties. Of note, several compounds in the series displayed relevant cytotoxicity, which warrants scrutiny while interpreting biological activities that have been reported for structurally related molecules. In addition, antiparasitic activities were recorded against a range of human-infective protozoa, including Trypanosoma cruzi , T. brucei rhodesiense , and Leishmania infantum . The most interesting compounds displayed low micromolar whole-cell potencies against individual or several parasitic species, while lacking cytotoxicity against human cells. |
