Scientists from Uruguay and the US have made new compounds that could be used to treat Chagas disease. Chagas disease is a parastic disease caused by the protozoan Trypanosoma cruzi. It affects an estimated 10 million people in South and Central America and results in 20 000 deaths each year.
The cysteine protease cruzipain is an essential T. cruzi enzyme and is one of the few validated drug targets for the disease. Current treatments include Nifurtimox and Benznidazole, but the cruzipain is becoming resistant to them.
Thiosemicarbazones have been described as cruzipain inhibitors. Now, the team have replaced the sulfur in these compounds with selenium to make selenosemicarbazones to find new drug leads. The selenosemicarbazones showed enhanced cysteine protease inhibitory activity compared to the thiosemicarbazones and to Benznidazole, one of the two current drugs on the market.
Selenosemicarbazones as Potent Cruzipain Inhibitors and their Antiparasitic Properties against Trypanosoma cruzi
Chiara Pizzo, Paula Faral-Tello, Gustavo Salinas, Martín Fló, Carlos Robello, Peter Wipf and Graciela Mahler
Med. Chem. Commun., 2011, Accepted Manuscript
Research on the Chagas and neglected diseases was also recently the subject of MedChemComm‘s latest poster prize.