In vitro and in vivo anti-Leishmania activity of polysubstituted synthetic chalcones

被引：53

作者：

Aponte, Jose C. ^{[2
]}

Castillo, Denis ^{[3
]}

Estevez, Yannick ^{[1
,4
]}

Gonzalez, German ^{[3
]}

Arevalo, Jorge ^{[3
]}

Hammond, Gerald B. ^{[2
]}

Sauvain, Michel ^{[1
,4
]}

机构：

[1] Univ Toulouse 3, IRD, UMR 152, Mission IRD, Lima, Peru

[2] Univ Louisville, Dept Chem, Louisville, KY 40292 USA

[3] Univ Peruana Cayetano Heredia, Inst Med Trop Alexander von Humboldt, Lima, Peru

[4] Univ Toulouse, UPS, UMR 152, Lab Pharmacochim Subst Nat & Pharmacophores Redox, F-31062 Toulouse 9, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期

关键词：

Anti-Leishmanial drugs; Chalcone; Leishmania amazonensis; Peruviana; Braziliensis; RESISTANCE;

D O I：

10.1016/j.bmcl.2009.11.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：100 / 103

页数：4

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