Bisbenzamidines as antifungal agents. are both amidine functions required to observe an anti-Pneumocystis carinii activity?
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.
Laurent
Julien
J
Laboratory of Organic Chemistry, Faculty of Sciences, University of Mons-UMONS, 20 place du parc, B-7000 Mons, Belgium.
Stanicki
Dimitri
D
Huang
Tien L
TL
Dei-Cas
Eduardo
E
Pottier
Muriel
M
Aliouat
El Mouktar
el M
Vanden Eynde
Jean Jacques
JJ
D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001550:Benzamidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015394:Molecular Structure; D045363:Pneumocystis carinii / Q000187:drug effects*
D000935:Antifungal Agents; D001550:Benzamidines