The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1,3-5 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 (an up to) a thousand fold higher activity than the reference drug benznidazole and furthermore low cytotoxicity on rat myogenic L6 cells.
New promising compounds with in vitro nanomolar activity against Trypanosoma cruzi / Friggeri, Laura; Scipione, Luigi; Costi, Roberta; Marcel, Kaiser; Francesca, Moraca; Claudio, Zamperini; Botta, Bruno; DI SANTO, Roberto; DE VITA, Daniela; Reto, Brun; Tortorella, Silvano. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - STAMPA. - 4:(2013), pp. 538-541. [10.1021/ml400039r]
New promising compounds with in vitro nanomolar activity against Trypanosoma cruzi
FRIGGERI, LAURA;SCIPIONE, Luigi;COSTI, Roberta;BOTTA, Bruno;DI SANTO, Roberto;DE VITA, DANIELA;TORTORELLA, Silvano
2013
Abstract
The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1,3-5 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 (an up to) a thousand fold higher activity than the reference drug benznidazole and furthermore low cytotoxicity on rat myogenic L6 cells.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
