Artemisinin drugs antimalarial

Klayman DL. (1985) Qinghaosu (Artemisinin) — an antimalarial drug from China. Science 228 1049-1055. 

Vroman JA, Alvim-Gaston M, Avery MA. Current progress in the chemistry, medicinal chemistry and drug design of artemisinin based antimalarials. Curr. Pharm. Des. 1999 5 101-138. 

Burk, O., Arnold, K. A., Nussler, A. K., Schaeffeler, E., Efimova, E., Avery, B. A., Avery, M. A., Fromm M. F., and Eichelbaum, M. (2005) Antimalarial artemisinin drugs induce cytochrome P450 and MDR1 expression by activation of xenosensors pregnane X receptor and constitutive androstane receptor. Mol. Pharmacol. 67,1954-1964. 

Bhisutthibhan, J., Pan, X.-O., Hossler, P.A., Walker, D.J., Yowell, C.A., Carlton, J., Dame, J.B., and Meshnick, S.R. The plasmodium falciparum translationally controlled tumor protein homolog and its reaction with the antimalarial drug artemisinin, /. Biol. Chem., 273,16192,1998. 21. Avery, M.A., Chong, W.K.M., and Jennings-White, C. Stereoselective total synthesis of (+)-artemisinin, the antimalarial constituent of Artemisia annua L., /. Am. Chem. Soc., 114,974,1992. Avery, M.A., Bonk, J.D., and Bupp, J. Radiolabeled antimalarials synthesis of 14C-artemisinin, /. Labelled Comp. Radiopharm., 38, 263, 1996. 

Klayman, D. L., Qinghaosu (artemisinin) An antimalarial drug from China, Science, 228, 1049-1054 (1985). 

Price, R. N. 2000. Artemisinin drugs novel antimalarial agents . Expert Opin Investig Drugs. P(8) 1815-27. 

The synthesis of artemisinin, an antimalarial drug isolated from qinghao, a Chinese herbal remedy (Section 10.16)... 

Artensunate is a water-soluble derivative of artemisinin, an antimalarial drug given by injection. A common side effect is delayed haemolytic anaemia in patients with severe malaria, although it is unclear whether this is related to the drug or the disease. 

Artemisinin (20) Antimalarial drug significant anticancer effects effective against schistosomes... 

Antimalarial drug artemisinine, sesquiterpenic 8-lactone with 1,2,5-trioxane (endoperoxide) fragment 98CSR273. 

Trioxane 210 has been used as a model system by Gu and coworkers to study the antimalarial drug artemisinin 211 (Scheme 137) [97CPL234, 99JST103]. It is the boat/twist form rather than the chair conformer of 210 that describes the subunit in 211. Moreover, geometric parameters and vibrational frequencies can only reliably be computed at the DFT level and by post-Hartree-Fock methods. B3-LYP/6-31G calculations on the conformers of 3,3,6,6-tetramethyl-1,2,4,5-tetroxane show that the chair conformer is stabilized with respect to the twisted conformer by about -2.8 kcal/mol [00JST85]. No corresponding boat conformer was found. 

The Plasmodium falciparum malaria PD model successfully described the antimalarial effect of artemisinin, mefloquine, and a combination of the two drugs... 

WaUaart TE, Bouwmeester HJ, Hille J, Poppinga L, Maijers NCA (2001) Amorpha-4, 11-diene synthase cloning and functional expression of a key enzyme in the biosynthetic pathway of the novel antimalarial drug artemisinin. Planta 212 460-465... 

Other derivatives of artemisinin are in various stages of clinical development as antimalarial drugs in Europe. 

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