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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?

1, 1, 2, 3,4,5, 3,5, 3,5 and 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 / Revised: 1 June 2010 / Accepted: 7 June 2010 / Published: 11 June 2010
(This article belongs to the Special Issue ECSOC-13)
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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 pentamidine; Pneumocystis carinii; monobenzamidines
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Laurent, J.; Stanicki, D.; Huang, T.L.; Dei-Cas, E.; Pottier, M.; Aliouat, E.M.; Vanden Eynde, J.J. Bisbenzamidines as Antifungal Agents. Are Both Amidine Functions Required to Observe an Anti-Pneumocystis carinii Activity? Molecules 2010, 15, 4283-4293.

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