Seite - (000331) - in Biomedical Chemistry: Current Trends and Developments

Brandon S. Pybus* 3.4 Synthetic Vs. Natural Bioactive Compounds Against Tropical Disease 3.4.1 Introduction Tropical diseases, although largely neglected by the commercial pharmaceutical industry, are a major problem for people in poor and underdeveloped nations. Perhaps the most significant of these threats comes from malaria. Roughly half of the world’s population live in malaria endemic regions, and the WHO estimates that it caused 627,000 deaths in 2012 (CDC, August 18, 2014). Nearly 500 million cases of malaria are confirmed worldwide annually, with roughly 80% of those caused by Plasmodium vivax, a persistent strain of the parasite (Goncalves, 2014). Due to the constant emergence of resistance, there is an ongoing need for the development of new drugs for malaria (Rosenthal, 2003). For this reason, and in the interest of outlining a generic drug development paradigm in limited space, we will focus the topic of the current discussion on the historical successes and failures of natural products in treating malaria and the efforts in the modern era to combat drug resistance and poor drug tolerance with synthetic drugs. 3.4.2 Early History of Malaria Treatment; Quinine and Artemisinin “The angel of disease and death, ascending from his oozy bed, along the marshy margins of the bottom grounds […] floats in his aerial chariot, and in seasons favorable to his progress, spreads mortal desolation as he flies”, so it was written in an Ohio newspaper article from 1820 (Findley, 1968). From this quote one can see how parasitic disease plagued the early frontiersmen of the 19th century. However, the unhappy coexistence of humans and parasitic disease goes back much further into the past. In fact, the earliest recorded descriptions of a