Seite - (000345) - in Biomedical Chemistry: Current Trends and Developments

Figure 3.4.5: Artemisinin was identified as the active ingredient in sweet wormwood in the 1970s. Several synthetic artemisinins and other endoperoxides now exist for the treatment of malaria. Figure 3.4.6: Generic paradigm for drug discovery that uses ADME properties to down-select potential candidates prior to expensive and labor intensive animal modeling. Dashed lines indicate a screen that is not necessarily a mandatory gate, but which can aid in the interpretation of potential later stage failure. References Achan, J., Talisuna, A. O., Erhart, A., Yeka, A., Tibenderana, J. K., Baliraine, F. N., (2011). Quinine, an old anti-malarial drug in a modern world: Role in the treatment of malaria. Malaria Journal, 10, 144-2875-10-144. Andrews, K. T., Fisher, G., & Skinner-Adams, T. S. (2014). Drug repurposing and human parasitic protozoan diseases. International Journal for Parasitology. Drugs and Drug Resistance, 4(2), 95-111. Antoine, T., Fisher, N., Amewu, R., O’Neill, P. M., Ward, S. A., & Biagini, G. A. (2014). Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS- dependent depolarization of the membrane potential. The Journal of Antimicrobial Chemotherapy, 69(4), 1005-1016. Ashley, E. A., Dhorda, M., Fairhurst, R. M., Amaratunga, C., Lim, P., Suon, S., (2014). Spread of artemisinin resistance in plasmodium falciparum malaria. The New England Journal of Medicine, 371(5), 411-423. Bennett, J. W., Pybus, B. S., Yadava, A., Tosh, D., Sousa, J. C., McCarthy, W. F., (2013). Primaquine failure and cytochrome P-450 2D6 in plasmodium vivax malaria. The New England Journal of Medicine, 369(14), 1381-1382. CDC. (August 18, 2014). Malaria. Retrieved September, 9 2014, 2014, from http://www.cdc.gov/malaria