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

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

doi:10.3390/molecules15064283

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

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

Authors

Julien Laurent¹, Dimitri Stanicki, Tien L Huang, Eduardo Dei-Cas, Muriel Pottier, El Mouktar Aliouat, Jean Jacques Vanden Eynde

Affiliation

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

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antifungal Agents / chemical synthesis
Antifungal Agents / chemistry*
Antifungal Agents / pharmacology*
Benzamidines / chemical synthesis
Benzamidines / chemistry*
Benzamidines / pharmacology*
Molecular Structure
Pneumocystis carinii / drug effects*

Substances

Antifungal Agents
Benzamidines