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Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents. 2018
Francesco Saccoliti, and
Valentina Noemi Madia, and
Valeria Tudino, and
Alessandro De Leo, and
Luca Pescatori, and
Antonella Messore, and
Daniela De Vita, and
Luigi Scipione, and
Reto Brun, and
Marcel Kaiser, and
Pascal Mäser, and
Claudia Magalhaes Calvet, and
Gareth K Jennings, and
Larissa M Podust, and
Roberta Costi, and
Roberto Di Santo
Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma, p.le Aldo Moro 5, I-00185, Rome, Italy. Electronic address: francesco.saccoliti@uniroma1.it.
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.
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