Bisbenzamidines as Antifungal Agents. Are Both Amidine Functions Required to Observe an Anti-Pneumocystis carinii Activity?

Molecules

Julien Laurent¹  Dimitri Stanicki¹  Tien L. Huang¹  Eduardo Dei-Cas¹  Muriel Pottier¹  El Mouktar Aliouat¹ 

[1] ¹Laboratory of Organic Chemistry, Faculty of Sciences, University of Mons-UMONS, 20 place du parc, B-7000 Mons, Belgium

关键词: pentamidine;    Pneumocystis carinii;    monobenzamidines;   

DOI  :  10.3390/molecules15064283

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.