Recent Highlights in Anti‐infective Medicinal Chemistry from South Africa

Abstract

Global advancements in biological technologies have vastly increased the variety of and accessibility to bioassay platforms, while simultaneously improving our understanding of druggable chemical space. In the South African context, this has resulted in a rapid expansion in the number of medicinal chemistry programmes currently operating, particularly on university campuses. Furthermore, the modern medicinal chemist has the advantage of being able to incorporate data from numerous related disciplines into the medicinal chemistry process, allowing for informed molecular design to play a far greater role than previously possible. Accordingly, this review focusses on recent highlights in drug-discovery programmes, in which South African medicinal chemistry groups have played a substantive role in the design and optimisation of biologically active compounds which contribute to the search for promising agents for infectious disease.

Biological and Medicinal Chemistry in Africa

“…These same trends are evident in Africa, where the scope of science falling under the umbrella of chemical biology has expanded from traditional strengths in natural product chemistry, [8,9] organic chemistry, [10,11] and biochemistry, [12] into contemporary programs in enzymology, [13] biocatalysis, [14] bioinorganic chemistry, [15] medicinal chemistry and drug discovery [16,17] …”

“…These same trends are evident in Africa, where the scope of science falling under the umbrella of chemical biology has expanded from traditional strengths in natural product chemistry, [8,9] organic chemistry, [10,11] and biochemistry, [12] into contemporary programs in enzymology, [13] biocatalysis, [14] bioinorganic chemistry, [15] medicinal chemistry and drug discovery. [16,17] Given the high burden of neglected disease in Africa, [18] the proclivity of chemical biology projects to occur in the multidisciplinary healthcare space [19] make it a particularly important field in Africa. The population of Africa is the youngest, and fastest growing in the world, and harnessing the economic benefits of scientific research is seen as a critical element of sustained and equitable growth in the continent.…”

Medicinal Chemistry Out of Africa

“…1,2 Africa's extensive biological diversity and traditional remedies have previously highlighted terrestrial and marine bioactive natural products. 3 However, modern drug discovery approaches have recently driven African medicinal chemical research outputs in more universal, relevant, and exciting directions. Since African populations carry the brunt of global infectious diseases, it is unsurprising that most publications focus heavily on diseases caused by parasitic, microbial, and viral infections such as malaria, leishmaniasis, tuberculosis, and HIV.…”

“…This is alarming given the fact that Africa bears over 20% of the world’s disease burden. Furthermore, scientific output from Africa represents less than 1% of the global share and disproportionately emerges from South Africa and Egypt, where academic institutions as well as science and technology receive significantly more attention compared with other African nations. , Africa’s extensive biological diversity and traditional remedies have previously highlighted terrestrial and marine bioactive natural products . However, modern drug discovery approaches have recently driven African medicinal chemical research outputs in more universal, relevant, and exciting directions.…”