by Winge T, Imberg I, Perry B, Matheeussen A, Caljon G, Kalinin D, Wünsch B. ChemMedChem 2024, 19: e202400220. doi: 10.1002/cmdc.202400220
Summary: The authors of this manuscript report on the synthesis and antileishmanial and antitrypanosomal activity of a series of pyrazoles and triazoles. In order to broaden the structure activity relationships for pyrazoles with antileishmanial and antitrypanosomal activity, a set of 15 compounds was prepared and pharmacologically evaluated. None of these compounds had discernable activity against L. infantum but some had promising antitrypanosomal activity with IC50 values in the low micromolar range. Unfortunately, the most potent antitrypanosomal compound in this study was toxic to primary peritoneal mouse macrophages and MRC-5 human fibroblast cells. Further studies with this compound class should aim to increase antileishmanial and/or antitrypanosomal activity while reducing unspecific toxicity. This project was performed within DNDi’s Open Synthesis Network.
