About 50 years after their development, the benzimidazole anthelmintic drugs still occupy a key role in the treatment of parasitic diseases. Like other anti-infective drugs, their extensive use has led to resistance development and now requires new solutions to treat these diseases. Organometallic derivatization of existing drugs has become a common strategy to design new drug candidates, which could benefit from enhanced activity against resistant or sensitive strains through the incorporation of an organometallic fragment. In this study, we describe the development of a new series of organometallic derivatives of benzimidazole anthelmintics. Ten derivatives, six of which were organometallic, were synthesized and characterized. In silico and in vitro studies were performed to determine their biological activity. Therefore, they were screened against a range of nematodes and other parasites. Biological activities were found for some of the derivatives against Strongyloides ratti, Ancylostoma ceylanicum, Trichuris muris, Schistosoma mansoni, Echinococcus multilocularis, or Leishmania infantum in similar ranges as the parent anthelmintics. Even if the activity of the benzimidazole scaffold was not systematically enhanced, this strategy is a good starting point for the development of new antiparasitic compounds and for further study of the mode of action of these drugs.
BT - Chembiochem : a European journal of chemical biology C1 - https://www.ncbi.nlm.nih.gov/pubmed/42571638 DA - 08/2026 DO - 10.1002/cbic.70490 IS - 15 J2 - Chembiochem LA - ENG M3 - Article N2 -About 50 years after their development, the benzimidazole anthelmintic drugs still occupy a key role in the treatment of parasitic diseases. Like other anti-infective drugs, their extensive use has led to resistance development and now requires new solutions to treat these diseases. Organometallic derivatization of existing drugs has become a common strategy to design new drug candidates, which could benefit from enhanced activity against resistant or sensitive strains through the incorporation of an organometallic fragment. In this study, we describe the development of a new series of organometallic derivatives of benzimidazole anthelmintics. Ten derivatives, six of which were organometallic, were synthesized and characterized. In silico and in vitro studies were performed to determine their biological activity. Therefore, they were screened against a range of nematodes and other parasites. Biological activities were found for some of the derivatives against Strongyloides ratti, Ancylostoma ceylanicum, Trichuris muris, Schistosoma mansoni, Echinococcus multilocularis, or Leishmania infantum in similar ranges as the parent anthelmintics. Even if the activity of the benzimidazole scaffold was not systematically enhanced, this strategy is a good starting point for the development of new antiparasitic compounds and for further study of the mode of action of these drugs.
PY - 2026 SP - 1 EP - 16 T2 - Chembiochem : a European journal of chemical biology TI - Synthesis and Antiparasitic Activities of New Organometallic Derivatives of the Benzimidazole Anthelmintic Drugs. UR - https://pmc.ncbi.nlm.nih.gov/articles/PMC13453072/pdf/CBIC-27-e70490.pdf VL - 27 SN - 1439-7633 ER -