Design and synthesis of amidoxime derivatives for orally potent C-alkylamidine-based antimalarial agents

被引：18

作者：

Ouattara, Mahama ^{[1
]}

Wein, Sharon ^{[2
]}

Denoyelle, Severine ^{[1
]}

Ortial, Stephanie ^{[1
]}

Durand, Thierry ^{[1
]}

Escale, Roger ^{[1
]}

Vial, Henri ^{[2
]}

Vo-Hoang, Yen ^{[1
]}

机构：

[1] Univ Montpellier 2, Univ Montpellier 1, CNRS, UMR 5247,Inst Biomol Max Mousseron, F-34093 Montpellier, France

[2] Univ Montpellier 2, CNRS, UMR 5235, F-34095 Montpellier, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 03期

关键词：

C-Alkylamidine; Design of prodrug; Specific O-substitutions; Alkylamidoxime; Clearance of parasitemia; Oral antimalarial agent; PHOSPHOLIPID-METABOLISM; SALTS; PRODRUGS; PENTAMIDINE; ANTAGONISTS; REDUCTION; MOLECULES; AMIDINES;

D O I：

10.1016/j.bmcl.2008.12.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Within the frame of the design of prodrug candidates to deliver a C-alkylamidine antimalarial agent, we showed that specific O-substitutions were needed on the alkylamidoxime structure. Among the newly synthesized molecules, bis-oxadiazolone and bis-O-methylsulfonylamidoxime derivatives induced a complete clearance of parasitemia in mice after oral administration. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：624 / 626

页数：3

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