Seite - (000340) - in Biomedical Chemistry: Current Trends and Developments

inexpensive drugs are far more likely in that regard to make a meaningful impact on the fight against parasitic disease worldwide. 3.4.5 Natural Products in the Treatment of Malaria As we have noted many of the progenitive compounds (quinine, artemisinin) for the treatment of malaria are naturally derived. Efforts continue to isolate natural compounds with anti-protozoal activity (Mohammed, 2014; Singh, 2014; Traore, 2014). Natural sources including plants, microbes, and animals provide libraries with rich chemical diversity, however, isolation and purification of active components presents a significant challenge in natural product development. The complexity of isolation is highly dependent on structure, which can often be quite complex with compounds isolated from natural sources. This of course leads to a second challenge for the development of natural products, namely synthesis. Once a hit is identified from a mixture, large quantities are often needed for further pre-clinical or clinical testing. The likelihood of identifying a clinic-ready compound from a natural source in today’s regulatory environment is small. The more likely scenario involves the identification of a hit compound, which can be potentially modified to improve drug-like characteristics or decrease potential liabilities from toxicity. As we will discuss in the next section, the source of starting material for a drug development project is largely irrelevant once a hit is identified, as all compounds should be gated through the same testing scheme to ensure the end product matches the target product profile. 3.4.6 Considerations for Anti-parasitic Drug Development In any drug candidate’s journey down a development pipeline there are many pitfalls. Sadly, activity against a biological target or even in vivo efficacy does not make a successful drug. Careful consideration should be given early to liabilities that might lead to late stage failure, which could be costly and drain resources vital to the discovery of a potential candidate. In 1991, the leading cause of attrition for drug candidates was