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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.

SUBMITTER: Friggeri L 

PROVIDER: S-EPMC4027138 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature

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

Friggeri Laura L   Scipione Luigi L   Costi Roberta R   Kaiser Marcel M   Moraca Francesca F   Zamperini Claudio C   Botta Bruno B   Di Santo Roberto R   De Vita Daniela D   Brun Reto R   Tortorella Silvano S  

ACS medicinal chemistry letters 20130507 6


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. ...[more]

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