In a collaboration with a consortium of companies and universities, Mercachem has worked on a project to convert human PDE4 inhibitors into Trypanosoma brucei PDEB1 inhibitors to develop a new drug for the treatment of African sleeping sickness. This resulted in several publications, one of which has just been published in the Journal of Medicinal Chemistry.
Johan Veerman (Senior Group Leader Medicinal Chemistry) says, “This article describes the synthesis and activity of the first compounds that are more selective for the T. brucei PDEB1, and several X-ray crystal structures show the compounds binding in the enzyme.”
Toine van den Bergh (Senior Scientist Medicinal Chemistry) adds, “It was great to be part of such a partnership. We could learn from each other, but above all contribute to finding a cure for the disease, which has affected many people.”
Further optimization of these compounds is ongoing at the Vrije Universiteit Amsterdam.
Think Mercachem for your next collaboration!