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

Pharmaceuticals

Dimitri Stanicki²  Muriel Pottier⁴  Nausicaa Gantois⁴  Claire Pinçon¹  Delphine Forge²  Isabelle Mahieu³  Sstien Boutry³  Jean Jacques Vanden Eynde²  Anna Martinez⁴  Eduardo Dei-Cas⁴ 

[1] EA2694, Department of Biostatistics, Université de Lille Nord de France, F-59000 Lille, France; E-Mail:;Laboratory of Organic Chemistry, University of Mons-UMONS, B-7000 Mons, Belgium; E-Mails:;Department of General, Organic, and Biomedical Chemistry, NMR and Molecular Imaging Laboratory, University of Mons-UMONS, B-7000 Mons, Belgium; E-Mails:;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; E-Mails:

关键词: Pneumocystis;    pentamidine;    diamidine;   

DOI  :  10.3390/ph6070837

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.