Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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3-Aminosterol Compounds as a New Class of Anti-Malarial Agents against Chloroquine-Susceptible and -Resistant Plasmodium falciparum

Author(s): Chanaz Salmi, Celine Loncle, Nicolas Vidal, Christophe Rogier, Yves Letourneux, Bruno Pradines, Jean Michel Brunel.

Abstract:

A series of 3-amino- and polyaminosterol analogues of squalamine and trodusquemine were evaluated for their in vitro antimalarial properties against chloroquine-susceptible and -resistant Plasmodium falciparum. These derivatives were designed possessing a good therapeutic index compared to chloroquine with IC50 varying from 2 to 22 μM. These compounds as well as the underlying design rationale may find usefulness in the discovery and development of new antimalarial drugs.

Keywords: Squalamine, Trodusquemine, Aminosterol derivatives, Antimalarial activity

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Article Details

VOLUME: 6
ISSUE: 2
Year: 2009
Page: [163 - 166]
Pages: 4
DOI: 10.2174/157018009787582633
Price: $58