Author | Saccoliti, Francesco | |
Author | Madia, Valentina Noemi | |
Author | Tudino, Valeria | |
Author | De Leo, Alessandro | |
Author | Pescatori, Luca | |
Author | Messore, Antonella | |
Author | De Vita, Daniela | |
Author | Scipione, Luigi | |
Author | Brun, Reto | |
Author | Kaiser, Marcel | |
Author | Mäser, Pascal | |
Author | Calvet, Claudia Magalhaes | |
Author | Jennings, Gareth K. | |
Author | Podust, Larissa M. | |
Author | Costi, Roberta | |
Author | Di Santo, Roberto | |
Access date | 2018-08-30T15:10:25Z | |
Available date | 2018-08-30T15:10:25Z | |
Document date | 2018 | |
Citation | SACCOLITI, Francesco; et al. Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents. European Journal of Medicinal Chemistry, v.156, p.53-60, June 2018. | pt_BR |
ISSN | 0223-5234 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/28472 | |
Language | eng | pt_BR |
Publisher | Elsevier | pt_BR |
Rights | restricted access | pt_BR |
Subject in Portuguese | Antifúngicos | pt_BR |
Subject in Portuguese | Antitripanossomal | pt_BR |
Subject in Portuguese | Antiplasmodial | pt_BR |
Subject in Portuguese | Antileishmanial | pt_BR |
Subject in Portuguese | estudos in vivo | pt_BR |
Title | Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents | pt_BR |
Type | Article | pt_BR |
DOI | 10.1016/j.ejmech.2018.06.063 | |
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. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Swiss Tropical and Public Health Institute. Basel, Switzerland. | pt_BR |
Affilliation | Swiss Tropical and Public Health Institute. Basel, Switzerland. | pt_BR |
Affilliation | Swiss Tropical and Public Health Institute. Basel, Switzerland. | pt_BR |
Affilliation | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. San Diego, La Jolla, CA, USA / Fundação Oswaldo Cruz. Instituto Oswaldo cruz. Laboratório de Ultraestrutura Celular. Ri de Janeiro, RJ, Brasil. | pt_BR |
Affilliation | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. San Diego, La Jolla, CA, USA. | pt_BR |
Affilliation | University of California San Diego. Skaggs School of Pharmacy and Pharmaceutical Sciences. San Diego, La Jolla, CA, USA. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Affilliation | Istituto Pasteur-Fondazione Cenci Bolognetti. Dipartimento di Chimica e Tecnologie del Farmaco. “Sapienza” Università di Roma. Rome, Italy. | pt_BR |
Subject | Azole | pt_BR |
Subject | Antitrypanosomal | pt_BR |
Subject | Antiplasmodial | pt_BR |
Subject | Antileishmanial | pt_BR |
Subject | Antifungal | pt_BR |
Subject | CYP51 | pt_BR |
Subject | In vivo studies | pt_BR |
DeCS | Antifúngicos | pt_BR |
DeCS | Inibidores de 14-alfa Desmetilase | pt_BR |
e-ISSN | 1768-3254 | |
Embargo date | 2030-01-01 | |