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New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.

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 3 Silvano Tortorella 1
* Corresponding author
1 Dipartimento di Chimica e Tecnologie del Farmaco
2 Department of Medicinal Chemistry and Technologies
3 MPI - Medical Parasitology and Infection Biology [Basel, Suisse]
4 Dipartimento di Biotecnologie, Chimica e Farmacia
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 : Chagas disease CYP51 Trypanosoma cruzi aminopyridine antiparasitic activity azole
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Laura Friggeri, Luigi Scipione, Roberta Costi, Marcel Kaiser, Francesca Moraca, et al.. New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.. ACS Medicinal Chemistry Letters, American Chemical Society, 2013, 4 (6), pp.538-41. ⟨10.1021/ml400039r⟩. ⟨pasteur-01054197⟩

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