Title of article
Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine
Author/Authors
Maniyan Padmanilayam، نويسنده , , Bernard Scorneaux، نويسنده , , Yuxiang Dong، نويسنده , , Jacques Chollet، نويسنده , , Hugues Matile، نويسنده , , Susan A. Charman، نويسنده , , Darren J. Creek، نويسنده , , William N. Charman، نويسنده , , Josefina Santo Tomas، نويسنده , , Christian Scheurer، نويسنده , , Sergio Wittlin، نويسنده , , Reto Brun، نويسنده , , Jonathan L. Vennerstrom، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
5542
To page
5545
Abstract
With an aim to identify a dispiro-1,2,4-trioxolane with high oral activity and good physicochemical properties, 27 derivatives of an achiral piperidine trioxolane were synthesized; most were potent antimalarial peroxides with IC50s ranging from 0.20 to 7.0 ng/mL. The oral efficacies of two of these were superior to artesunate and comparable to artemether. The attractive chemical simplicity of these compounds is balanced only by an apparent metabolic susceptibility.
Keywords
Artemisinin , 2 , 1 , Secondary ozonide , Antimalarial , 4-Trioxolane
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797424
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