New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi

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• 作者：Laura Friggeri ; Luigi Scipione ; Roberta Costi ; Marcel Kaiser ; Francesca Moraca ; Claudio Zamperini ; Bruno Botta ; Roberto Di Santo ; Daniela De Vita ; Reto Brun ; Silvano Tortorella
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：June 13, 2013
• 年：2013
• 卷：4
• 期：6
• 页码：538-541
• 全文大小：258K
• 年卷期：v.4,no.6(June 13, 2013)
• ISSN：1948-5875

文摘

The antiparasitic activity of azole and new 4-aminopyridine derivatives has been investigated. The imidazoles 1 and 3鈥?b>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:

Trypanosoma cruzi; CYP51; antiparasitic activity; Chagas disease; azole; aminopyridine