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Pharmaceuticals 2013, 6(7), 837-850; doi:10.3390/ph6070837
Article

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

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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)
View Full-Text   |   Download PDF [428 KB, 3 July 2013; original version 1 July 2013]   |   Browse Figures

Abstract

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.
Keywords: Pneumocystis; pentamidine; diamidine Pneumocystis; pentamidine; diamidine
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Stanicki, D.; Pottier, M.; Gantois, N.; Pinçon, C.; Forge, D.; Mahieu, I.; Boutry, S.; Eynde, J.J.V.; 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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