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

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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 μg/mL of 87% and 96%, respectively. Those compounds remained active at 0.1 μg/mL.

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Laurent, J., Stanicki, D., Huang, T. L., Dei-Cas, E., Pottier, M., Aliouat, E. M., & Vanden Eynde, J. J. (2010). Bisbenzamidines as antifungal agents. Are both amidine functions required to observe an anti-Pneumocystis carinii activity? Molecules, 15(6), 4283–4293. https://doi.org/10.3390/molecules15064283

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