In vitro and in vivo anti-Leishmania activity of polysubstituted synthetic chalcones.
The in vitro screening of 43 polysubstituted chalcones against Leishmania amazonensis axenic amastigotes, led to the evaluation of 9 of them in a macrophage-infected model with the two other most infectious Leishmania species prevalent in Peru (L. braziliensis and L. peruviana). The five most active and selective chalcones were studied in vivo, resulting on the identification of two chalcones with high reduction parasite burden percentages.
Aponte
José C
JC
Department of Chemistry, University of Louisville, KY 40292, USA.
Castillo
Denis
D
Estevez
Yannick
Y
Gonzalez
German
G
Arevalo
Jorge
J
Hammond
Gerald B
GB
Sauvain
Michel
M
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D047188:Chalcones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007891:Leishmania / Q000187:drug effects; D008264:Macrophages / Q000469:parasitology; D051379:Mice; D008807:Mice, Inbred BALB C; D021261:Parasitic Sensitivity Tests
D000981:Antiprotozoal Agents; D047188:Chalcones