Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents

European Journal of Medicinal Chemistry
Francesco SaccolitiRoberto Di Santo

Abstract

We discovered a series of azole antifungal compounds as effective antiprotozoal agents. They displayed promising inhibitory activities within the micromolar-submicromolar range against P. falciparum, L. donovani, and T. b. rhodesiense. Moreover, most of such compounds showed excellent nanomolar IC50 against T. cruzi, showing also very low cytotoxicity. Discussion of structure-activity relationships and biological data for these compounds are provided against the different parasites. To assess the mechanism of action against T. cruzi we proved that the most potent compounds (3b, 3j-l) inhibited the T. cruzi CYP51. Moreover, the most active derivative 3j dramatically reduced parasitemia in T. cruzi mouse model without acute toxicity.

Citations

Apr 28, 2019·Molecular Diversity·Nima Razzaghi-AslMohammad Johari-Ahar
Feb 24, 2020·European Journal of Medicinal Chemistry·Fanny MathiasPatrice Vanelle
Aug 8, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Valentina Noemi MadiaAntonella Messore
Feb 18, 2021·Current Pharmaceutical Design·Aline A Zuma, Wanderley de Souza

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