Structure-activity relationships of the antimalarial agent artemisinin. 7. Direct modification of (+)-artemisinin and in vivo antimalarial screening of new, potential …

MA Avery, M Alvim-Gaston, JA Vroman…

Index: Avery, Mitchell A.; Alvim-Gaston, Maria; Vroman, Jeffrey A.; Wu, Baogen; Ager, Arba; Peters, Wallace; Robinson, Brian L.; Charman, William Journal of Medicinal Chemistry, 2002 , vol. 45, # 19 p. 4321 - 4335

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Citation Number: 67

Abstract

On the basis of earlier reported quantitative structure-activity relationship studies, a series of 9β-16-(arylalkyl)-10-deoxoartemisinins were proposed for synthesis. Several of the new compounds 7 and 10-14 were synthesized employing the key synthetic intermediate 23. In a second approach, the natural product (+)-artemisinic acid was utilized as an acceptor for conjugate addition, and the resultant homologated acids were subjected to singlet ...