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• Laurent, J
• Stanicki, D
• Huang, T
• Dei-Cas, E
• Pottier, M
• Aliouat, E
• Vanden Eynde, J
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• Laurent, J
• Stanicki, D
• Huang, T
• Dei-Cas, E
• Pottier, M
• Aliouat, E
• Vanden Eynde, J
• [+] on PubMed
• Laurent, J
• Stanicki, D
• Huang, T
• Dei-Cas, E
• Pottier, M
• Aliouat, E
• Vanden Eynde, J

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Molecules 2010, 15(6), 4283-4293; doi:10.3390/molecules15064283

Article

Bisbenzamidines as Antifungal Agents. Are Both Amidine Functions Required to Observe an Anti-Pneumocystis carinii Activity?

Julien Laurent ¹ , Dimitri Stanicki ¹ , Tien L. Huang ² , Eduardo Dei-Cas ^3,4,5 , Muriel Pottier ^3,5 , El Mouktar Aliouat ^3,5  and Jean Jacques Vanden Eynde ^1,*

¹ Laboratory of Organic Chemistry, Faculty of Sciences, University of Mons-UMONS, 20 place du parc, B-7000 Mons, Belgium ² Division of Basic Pharmaceutical Sciences, College of Pharmacy, Xavier University of Louisiana, 1 Drexel drive, New Orleans, LA 70125, USA ³ Department of Parasitology-Mycology, Faculty of Biological and Pharmaceutical Sciences, University of Lille Nord de France, Lille, France ⁴ Department of Parasitology-Mycology, Faculty of Medicine, University of Lille Nord de France, Biology-Pathology Centre, University Hospital Center, Lille, France ⁵ Biology and Diversity of Emergent Eukaryotic Pathogens (BDEEP) (EA3609), IFR142, Institut Pasteur de Lille, Lille, France

* Author to whom correspondence should be addressed.

Received: 26 May 2010; in revised form: 1 June 2010 / Accepted: 7 June 2010 / Published: 11 June 2010

(This article belongs to the Special Issue ECSOC-13)

Download PDF Full-Text [126 KB, uploaded 14 June 2010 08:24 CEST]

Abstract: A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 µg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 µg/mL.

Keywords: pentamidine; Pneumocystis carinii; monobenzamidines

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