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)

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

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

Domains: Life Sciences [q-bio]; Pharmaceutical sciences; Pharmacology; Life Sciences [q-bio]; Microbiology and Parasitology; Parasitology

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, 2013, 4 (6), pp.538-41. ⟨10.1021/ml400039r⟩. ⟨pasteur-01054197⟩