Two-Step Synthesis of Achiral Dispiro-1, 2, 4, 5-tetraoxanes with Outstanding Antimalarial Activity, Low Toxicity, and High-Stability Profiles†

…, D Stanford, P Gibbons, J Davies, L Vivas…

文献索引：Ellis, Gemma L.; Amewu, Richard; Sabbani, Sunil; Stocks, Paul A.; Shone, Alison; Stanford, Deborah; Gibbons, Peter; Davies, Jill; Vivas, Livia; Charnaud, Sarah; Bongard, Emily; Hall, Charlotte; Rimmer, Karen; Lozanom, Sonia; Jesus, Maria; Gargallo, Domingo; Ward, Stephen A.; O'Neill, Paul M. Journal of Medicinal Chemistry, 2008 , vol. 51, # 7 p. 2170 - 2177

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被引用次数: 54

摘要

A rapid, two-step synthesis of a range of dispiro-1, 2, 4, 5-tetraoxanes with potent antimalarial activity both in vitro and in vivo has been achieved. These 1, 2, 4, 5-tetraoxanes have been proven to be superior to 1, 2, 4-trioxolanes in terms of stability and to be superior to trioxane analogues in terms of both stability and activity. Selected analogues have in vitro nanomolar antimalarial activity and good oral activity and are nontoxic in screens for both ...