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

Author(s): Dimitri Stanicki | Muriel Pottier | Nausicaa Gantois | Claire Pinçon | Delphine Forge | Isabelle Mahieu | Sébastien Boutry | Jean Jacques Vanden Eynde | Anna Martinez | Eduardo Dei-Cas | El-Moukhtar Aliouat

Journal: Pharmaceuticals
ISSN 1424-8247

Volume: 6;
Issue: 7;
Start page: 837;
Date: 2013;
Original page

Keywords: Pneumocystis | pentamidine | diamidine

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.
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