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Biological evaluation and structure-activity relationships of imidazole-based compounds as antiprotozoal agents.
Saccoliti, Francesco; Madia, Valentina Noemi; Tudino, Valeria; De Leo, Alessandro; Pescatori, Luca; Messore, Antonella; De Vita, Daniela; Scipione, Luigi; Brun, Reto; Kaiser, Marcel; Mäser, Pascal; Calvet, Claudia Magalhaes; Jennings, Gareth K; Podust, Larissa M; Costi, Roberta; Di Santo, Roberto.
Affiliation
  • Saccoliti F; 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.
  • Madia VN; 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: valentinanoemi.madia@uniroma1.it.
  • Tudino V; 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: valeria.tudino@uniroma1.it.
  • De Leo A; 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: alessandrodl93@gmail.com.
  • Pescatori L; 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: luca.pescatori@uniroma1.it.
  • Messore A; 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: antonella.messore@gmail.com.
  • De Vita D; 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: daniela.devita@uniroma1.it.
  • Scipione L; 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: luigi.scipione@uniroma1.it.
  • Brun R; Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002, Basel, Switzerland. Electronic address: reto.brun@unibas.ch.
  • Kaiser M; Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002, Basel, Switzerland. Electronic address: marcel.kaiser@swisstph.ch.
  • Mäser P; Swiss Tropical and Public Health Institute, Socinstrasse 57, CH-4002, Basel, Switzerland. Electronic address: pascal.maeser@swisstph.ch.
  • Calvet CM; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, CA, 92093, USA; Laboratório de Ultraestrutura Celular, Instituto Oswaldo Cruz, FIOCRUZ, Rio de Janeiro, RJ, 21040-360, Brazil. Electronic address: claudiacalvet@gmail.com.
  • Jennings GK; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, CA, 92093, USA. Electronic address: gjennings@ucsd.edu.
  • Podust LM; Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California San Diego, La Jolla, CA, 92093, USA. Electronic address: lpodust@ucsd.edu.
  • Costi R; 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: roberta.costi@uniroma1.it.
  • Di Santo R; 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: roberto.disanto@uniroma1.it.
Eur J Med Chem ; 156: 53-60, 2018 Aug 05.
Article in En | MEDLINE | ID: mdl-30006174
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Trypanosoma cruzi / Chagas Disease / Imidazoles / Antiprotozoal Agents Limits: Animals / Female / Humans Language: En Journal: Eur J Med Chem Year: 2018 Document type: Article
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Trypanosoma cruzi / Chagas Disease / Imidazoles / Antiprotozoal Agents Limits: Animals / Female / Humans Language: En Journal: Eur J Med Chem Year: 2018 Document type: Article