title: New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.
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.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Laura
authors.initials: L
authors.lastname: Friggeri
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Luigi
authors.initials: L
authors.lastname: Scipione
authors.affiliation: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Roberta
authors.initials: R
authors.lastname: Costi
authors.affiliation: Department Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute , Socinstrasse 57, CH-4051 Basel, Switzerland.
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.affiliation: Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , Via A. Moro 2, 53100 Siena, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: Moraca
authors.affiliation: Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena , Via A. Moro 2, 53100 Siena, Italy.
authors.forename: Claudio
authors.initials: C
authors.lastname: Zamperini
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Bruno
authors.initials: B
authors.lastname: Botta
authors.affiliation: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Roberto
authors.initials: R
authors.lastname: Di Santo
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Daniela
authors.initials: D
authors.lastname: De Vita
authors.affiliation: 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.
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, "Sapienza" Università di Roma , P.le A. Moro 5, 00185 Rome, Italy.
authors.forename: Silvano
authors.initials: S
authors.lastname: Tortorella
keywords: CYP51; Chagas disease; Trypanosoma cruzi; aminopyridine; antiparasitic activity; azole