They’re an annoyance we’ve all undoubtedly had to face at some time, if not every day of our lives. Mosquitoes. Pesky little insects who, in this part of the world, are responsible mostly just for itchy arms and legs. In Africa, Central America, and Southeast Asia, though, their irritating bites often harbor something much more sinister. Malaria is a parasite-caused disease that infects between 300 and 500 million people worldwide. It accounts for nearly a half million deaths every year, making it the 5th-leading cause of death in the underdeveloped world and the 17th-leading cause worldwide. The disease is most prevalent in the tropics, a geographical region that also includes many of the poorest countries in the world. The parasite is spread primarily via a certain type of mosquito – females of the Anopheles genus – which is ubiquitous worldwide but especially in the tropics. The disease takes its highest toll in poor tropical countries, as previously mentioned, but also among its youngest victims.
Some progress has been made in disease control and prevention. An early attempt to control the spread of malaria came with the use of DDT, an insecticide intended to kill off many malaria-spreading mosquitoes. However, use of DDT was halted in 1972 due to its declining effectiveness as well as the FDA’s concern with its toxicity. Current disease control centers largely on preventing mosquito bites. Currently, many charities send mosquito nets to disease-ridden countries to help reduce the likelihood of being bitten, and therefore of contracting the disease. Those who are infected can be treated with different types of drugs, but these are often met with limited success.
The most popular antimalarial drug is chloroquine, which has been in use for over half a century. As is common with many antibiotics, however, many strains of malaria parasite have developed resistance to chloroquine. While malaria remains an enormous worldwide problem, further research on anti-malarial drugs remains limited. As malaria is generally concentrated in poorer regions of the world, pharmaceutical companies are unable to make much, if any, profit from the development and sale of new anti-malarial drugs. The brunt of anti-malarial research therefore falls to academic chemists. One particular drug was developed to treat those infected, called amodiaquine. Amodiaquine is a potent antibiotic used for the treatment of malaria, but, until now, its efficacy has been outweighed by its toxic side effects.
Enter Habiba Vaghoo, a second-year tenure track organic chemistry professor at Colorado College. Dr. Vaghoo’s subspecialties include fluorine chemistry and microwave synthesis, both of which are taken advantage of the synthesis of a novel anti-malarial drug. This new drug is very similar to amodiaquine, with the addition of a fluorine group being the only difference. By replacing certain parts of the amodiaquine molecule with fluorine analogs, the compound should become much less toxic while still remaining active against the malaria parasite. The proposed synthesis of this antibiotic may sound promising, but scientific research, especially the synthesis of new drugs, moves very slowly. Progress is being made, however. The first three steps of the eight-step synthesis have been performed successfully, and we first-block research students are hard at work on the fourth. It may seem difficult, but Dr. Vaghoo, along with a small crew of research students and her trusty robotic microwave, cleverly nicknamed Mr. Roboto by these writers, are closer than ever to treating malaria effectively and safely.
Nick Stevens and Josh Arguello