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
Letters in Drug Design & Discovery
Title: 3-Aminosterol Compounds as a New Class of Anti-Malarial Agents against Chloroquine-Susceptible and -Resistant Plasmodium falciparum
Volume: 6 Issue: 2
Author(s): Chanaz Salmi, Celine Loncle, Nicolas Vidal, Christophe Rogier, Yves Letourneux, Bruno Pradines and Jean Michel Brunel
Affiliation:
Keywords: Squalamine, Trodusquemine, Aminosterol derivatives, Antimalarial activity
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.
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Cite this article as:
Salmi Chanaz, Loncle Celine, Vidal Nicolas, Rogier Christophe, Letourneux Yves, Pradines Bruno and Brunel Michel Jean, 3-Aminosterol Compounds as a New Class of Anti-Malarial Agents against Chloroquine-Susceptible and -Resistant Plasmodium falciparum, Letters in Drug Design & Discovery 2009; 6 (2) . https://dx.doi.org/10.2174/157018009787582633
DOI https://dx.doi.org/10.2174/157018009787582633 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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