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

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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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) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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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