新型3,3,6,6-四烷基-1,2,4,5-四氧杂环己烷的合成及其抗疟活性
Synthesis and antimalarial activities of novel 3,3,6,6-tetraalkyl-1,2,4,5-tetraoxanes.
作者信息
Zmitek Katja, Stavber Stojan, Zupan Marko, Bonnet-Delpon Daniele, Charneau Sebastien, Grellier Phillipe, Iskra Jernej
机构信息
Laboratory of Organic and Bioorganic Chemistry, Jozef Stefan Institute and Faculty of Chemistry and Chemical Technology of University of Ljubljana, Jamova 39, 1000 Ljubljana, Slovenia.
出版信息
Bioorg Med Chem. 2006 Dec 1;14(23):7790-5. doi: 10.1016/j.bmc.2006.07.069. Epub 2006 Aug 17.
The oxidative system H2O2/fluorinated alcohol (TFE, HFIP) was used for direct acid- and MeReO3-catalyzed synthesis of 1,2,4,5-tetraoxanes from cyclic (C6, C7, and C12) and acyclic ketones. The influence of ring size and alkyl chain length were studied and antimalarial activities of synthetic 3,3,6,6-tetraalkyl-1,2,4,5-tetraoxanes were determined. Variations in their antimalarial activities were significant, although they share similar electrochemical properties of the peroxide bond.
氧化体系H2O2/氟化醇（TFE、HFIP）用于在酸和三氧化铼催化下，由环状（C6、C7和C12）和无环酮直接合成1,2,4,5-四氧六环。研究了环大小和烷基链长度的影响，并测定了合成的3,3,6,6-四烷基-1,2,4,5-四氧六环的抗疟活性。尽管它们的过氧键具有相似的电化学性质，但其抗疟活性的变化却很显著。
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