Making Medicines
Designing new medicines from scratch
hydroxychloroquine
Hydroxychloroquine is an anti-parastic and anti-inflammatory medicine. It was originally developed for the treatment of malaria, but it also has important anti-inflammatory abilities and is thus used for a wide range of other diseases.
The story of hydroxychloroquine starts in 1891 in the laboratory of Paul Ehrlich in Germany. His group used a drug called methylene blue to treat patients for malaria - the first synthetic drug used for the treatment of human malaria. Ehrlich's group successfully created an analogue of methylene blue by adding another side chain, which significantly improved the antimalarial activity.
Paul Ehrlich later went on to win the Novel Prize in Medicine (1908) for his contributions to immunology.
Over the next 120 years, a range of scientists from all over the world contributed to modifying the structure of methylene blue slightly to develop better and better medicines such as:
1925 - pamaquine
1930 - quinacrine (first widely used antimalarial - side effects included yellowing of the skin)
1930s - mepacrine
1934 - chloroquine
1955 - hydroxychloroquine
Starting point: Methylene Blue
Synthetic dye, absorbed by malaria parasites.
Currently used:
Chloroquine
Currently Used:
Hydroxychloroquine
3x less toxic than chloroquine
What similarities about the structure of the medicines above do you notice? What is the relevance of this?
Quinine
Notice the similarities in structure between the chloroquines above and this molecule.
Quinine is a natural product, derived from Cinchona calisaya tree.
First known use: Quechua people, Indigenous people of Peru, Bolivia and Ecuador.
It was used to treat malaria as early as 1632 by Spanish Jesuit missionaries who undoubtedly learned this from the Quechua people.
