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. 2010 Jun 11;15(6):4283-93.
doi: 10.3390/molecules15064283.

Bisbenzamidines as antifungal agents. are both amidine functions required to observe an anti-Pneumocystis carinii activity?

Julien Laurent  1 , Dimitri Stanicki, Tien L Huang, Eduardo Dei-Cas, Muriel Pottier, El Mouktar Aliouat, Jean Jacques Vanden Eynde
Affiliations

Bisbenzamidines as antifungal agents. are both amidine functions required to observe an anti-Pneumocystis carinii activity?

Julien Laurent et al. Molecules. .

Abstract

A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl- and N-hexyl-4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds, with inhibition percentages at 10.0 microg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 microg/mL.

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Figures

Figure 1
Figure 1
Structure of pentamidine (1) and piperazine-1, 4-bisbenzamidine (2).
Figure 2
Figure 2
General structure of the monobenzamidines 5-23 prepared in this study.
Scheme 1
Scheme 1
Synthesis of compounds 3-23.
See this image and copyright information in PMC

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