Metabolites of febrifugine and its synthetic analogue by mouse liver S9 and their antimalarial activity against Plasmodium malaria parasite

…, H Kikuchi, HS Kim, K Begum, Y Wataya…

文献索引：Kikuchi, Haruhisa; Tasaka, Hidehisa; Hirai, Shingo; Takaya, Yoshiaki; Iwabuchi, Yoshiharu; Ooi, Hidenori; Hatakeyama, Susumi; Kim, Hye-Sook; Wataya, Yusuke; Oshima, Yoshiteru Journal of Medicinal Chemistry, 2002 , vol. 45, # 12 p. 2563 - 2570

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被引用次数: 51

摘要

Quinazolinone type alkaloids, febrifugine (1) and isofebrifugine (2), isolated from Dichroa febrifuga roots, show powerful antimalarial activity against Plasmodium falciparum. Unfortunately, their emetic effect and other undesirable side effects have precluded their clinical use for malaria. Because of their antimalarial potency, analogues were searched for, with the goal of preserving the strong antimalarial activity, while dramatically reducing side ...