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In vitro activities of new 2-substituted quinolines against Leishmania donovani. 2011
Philippe M Loiseau, and
Suman Gupta, and
Aditya Verma, and
Saumya Srivastava, and
S K Puri, and
Faten Sliman, and
Marie Normand-Bayle, and
Didier Desmaele
Groupe Chimiothérapie Antiparasitaire, UMR 8076 CNRS BioCis, Faculté de Pharmacie, Université Paris-Sud, 92290-Châtenay-Malabry, France. philippe.loiseau@u-psud.fr
A series of 9 quinolines and 18 styrylquinolines was evaluated for the drugs' in vitro antileishmanial activities and cytotoxicities. The 7-aroylstyrylquinoline scaffold appeared to be the most promising one, with the most interesting compound, no. 35, exhibiting a 50% inhibitory concentration (IC(50)) of 1.2 μM and a selectivity index value of 121.5. Compound 35 was 10-fold and 8-fold more active than miltefosine and sitamaquine, the reference compounds, with selectivity indexes 607-fold and 60-fold higher, respectively.
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