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

Saccoliti, Francesco and Madia, Valentina Noemi and Tudino, Valeria and De Leo, Alessandro and Pescatori, Luca and Messore, Antonella and De Vita, Daniela and Scipione, Luigi and Brun, Reto and Kaiser, Marcel and Mäser, Pascal and Calvet, Claudia Magalhaes and Jennings, Gareth K. and Podust, Larissa M. and Costi, Roberta and Di Santo, Roberto. (2018) Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents. European journal of medicinal chemistry, 156. pp. 53-60.

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Official URL: https://edoc.unibas.ch/69262/

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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 IC; 50; 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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Brun, Reto and Kaiser, Marcel and Mäser, Pascal
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Elsevier
ISSN:0223-5234
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:05 Mar 2019 14:16
Deposited On:05 Mar 2019 14:16

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