Description and references

Active antimalarial constituent of the traditional Chinese medicinal herb Artemisia annua L., Compositae, which has been known for almost 2000 years as Qinghao. Isolated in 1972 and shown to be a sesquiterpene lactone with a peroxide moiety: K'o Hsueh T'ung Pao 22, 142 (1977), C.A. 87, 98788g (1977); L. Jing-Ming et al., Acta Chim. Sin. 37, 129 (1979), C.A. 92, 94594w (1980). Total synthesis and absolute configuration: G. Schmid, W. Hofheinz, J. Am. Chem. Soc. 105, 624 (1983). NMR spectral study: F. S. El-Feraly et al., Spectrosc. Lett. 18, 843 (1985). Antimalarial activity: Qinghaosu Antimalaria Coordinating Research Group, Chin. Med. J. 92, 811 (1979); L. J. Bruce-Chwatt, Br. Med. J. 284, 767 (1982). Clinical trials: J.-B. Jiang et al., Lancet 2, 285 (1982); W. Tongyin, X. Ruchang, J. Tradit. Chin. Med. 5, 240 (1985). Toxicity data: China Cooperative Research Group on Qinghaosu, ibid. 2, 31 (1982). Series of articles on chemistry, pharmacology, and antimalarial efficacy: ibid. 3-50. Brief reviews: H. Koch, Pharm. Int. 2, 184-185 (1981); D. L. Klayman, Science 228, 1049-1055 (1985). Review: R. N. Price, Expert Opin. Invest. Drugs 9, 1815-1827 (2000). Review of chemistry, pharmacology and clinical applications: X. D. Luo, C. C. Shen, Med. Res. Rev. 7, 29-52 (1987). Review of mechanism of action: S. R. Meshnick, Int. J. Parasitol. 32, 1655-1660 (2002).

Properties

Derivative