2. Academic Validation
  3. New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

  • ACS Med Chem Lett. 2013 May 7;4(6):538-41. doi: 10.1021/ml400039r.
Laura Friggeri 1,  Luigi Scipione 1,  Roberta Costi 2,  Marcel Kaiser 3,  Francesca Moraca 4,  Claudio Zamperini 4,  Bruno Botta 1,  Roberto Di Santo 2,  Daniela De Vita 1,  Reto Brun 5,  Silvano Tortorella 1
Affiliations

Affiliations

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
  • 2 Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
  • 3 Department Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute , Socinstrasse 57, CH-4051 Basel, Switzerland.
  • 4 Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , Via A. Moro 2, 53100 Siena, Italy.
  • 5 Department Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute , Socinstrasse 57, CH-4051 Basel, Switzerland ; University of Basel , Petersplatz 1, CH-4003 Basel, Switzerland.
PMID: 24900706 DOI: 10.1021/ml400039r
Abstract

The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1 and 3-5 showed a potent in vitro antichagasic activity with IC50 values in the low nanomolar concentration range. The (S)-1, (S)-3, and (S)-5 enantiomers showed (up to) a thousand-fold higher activity than the reference drug benznidazole and furthermore low cytotoxicity on rat myogenic L6 cells.

Keywords

CYP51; Chagas disease; Trypanosoma cruzi; aminopyridine; antiparasitic activity; azole.

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