by Winge T, Perry B, Matheeussen A, Caljon G, Wünsch B. ChemMedChem 2024, 19: e202400028. doi: 10.1002/cmdc.202400028
Summary: N-Pyrazolylcarboxamides and N-pyrazolylureas are promising lead compounds for the development of novel drugs against leishmaniasis. The authors of this manuscript report on the modification of 3-bromopyrazoles using Pd-catalyzed Sonogashira and Suzuki-Miyaura cross coupling reactions. A large set of pyrazoles with diverse aryl and alkynyl substituents was prepared and their activity against Leishmania and Trypanosoma parasites was determined. One compound showed some effectiveness against these parasites but also considerable toxicity against primary peritoneal mouse macrophages and MRC-5 human fibroblast cells; this small gap between desired antiparasitic activity and undesired cytotoxicity indicates low selectivity. This project was performed within DNDi’s Open Synthesis Network.
