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Pharmaceuticals 2013, 6(7), 837-850;

Diamidines versus Monoamidines as Anti-Pneumocystis Agents: An in Vivo Study

Laboratory of Organic Chemistry, University of Mons-UMONS, B-7000 Mons, Belgium
Biology & Diversity of Emerging Eukaryotic Pathogens (BDEEP), Center for Infection and Immunity of Lille (CIIL), INSERM U1019, CNRS UMR 8204, EA-4547, Univ Lille Nord de France, UDSL, Institut Pasteur de Lille, F-59000 Lille, France
EA2694, Department of Biostatistics, Université de Lille Nord de France, F-59000 Lille, France
Department of General, Organic, and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons-UMONS, B-7000 Mons, Belgium
CHU Lille, Biology & Pathology Center, Parasitology-Mycology, F-59000 Lille, France
Author to whom correspondence should be addressed.
Received: 22 April 2013 / Revised: 14 May 2013 / Accepted: 17 June 2013 / Published: 1 July 2013
(This article belongs to the Special Issue Antimicrobial Agents)
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Some compounds articulated around a piperazine or an ethylenediamine linker have been evaluated in vitro to determine their activity in the presence of a 3T6 fibroblast cell line and an axenic culture of Pneumocystis carinii, respectively. The most efficient antifungal derivatives, namely N,N′-bis(benzamidine-4-yl)ethane-1,2-diamine (compound 6, a diamidine) and N-(benzamidine-4-yl)-N′-phenylethane-1,2-diamine (compound 7, a monoamidine), exhibited no cytotoxicity and were evaluated in vivo in a rat model. Only the diamidine 6 emerged as a promising hit for further studies. View Full-Text
Keywords: Pneumocystis; pentamidine; diamidine Pneumocystis; pentamidine; diamidine

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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Stanicki, D.; Pottier, M.; Gantois, N.; Pinçon, C.; Forge, D.; Mahieu, I.; Boutry, S.; Vanden Eynde, J.J.; Martinez, A.; Dei-Cas, E.; Aliouat, E.-M. Diamidines versus Monoamidines as Anti-Pneumocystis Agents: An in Vivo Study. Pharmaceuticals 2013, 6, 837-850.

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