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

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'-...

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Main Authors: El-Moukhtar Aliouat (Author), Eduardo Dei-Cas (Author), Anna Martinez (Author), Jean Jacques Vanden Eynde (Author), Sébastien Boutry (Author), Isabelle Mahieu (Author), Delphine Forge (Author), Claire Pinçon (Author), Dimitri Stanicki (Author), Muriel Pottier (Author), Nausicaa Gantois (Author)
Format: Book
Published: MDPI AG, 2013-07-01T00:00:00Z.
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Summary: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.
Item Description:10.3390/ph6070837
1424-8247

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