Medicinal Chemistry Approaches to Tuberculosis and Trypanosomiasis

Some of the more recent efforts in tuberculosis (TB) and trypanosomiasis drug discovery from both Product Development Partnerships (PDPs) and academia are highlighted in this this volume. Drug discovery approaches include both target- and phenotypic whole cell screening- approaches. Regarding the latter, mechanism of action studies through target identification are also illustrated.

Provides an overview of the status of some of the current novel compounds in development as well as new emerging treatment options targeting novel mechanisms of actionIdentification of hits from phenotypic whole cell screening, followed by target identificationStrategies aimed at improving the efficacy of existing clinically used anti-TB drugs by taking advantage inhibitors of mycobacterial transcriptional regulators to boost the anti-tubercular activity, and circumvent acquired-resistance

1. Tuberculosis Steven J. Berthel, Christopher B. Cooper and Nader P. Fotouhi 2. Antituberculosis agents: Beyond medicinal chemistry rules Marco Pieroni 3. Development of MmpL3 inhibitors for tuberculosis treatment Giovanna Poce, Sara Consalvi, Giulia Venditti, Cristina Scarpecci and Mariangela Biava 4. Inhibitors of enzymes in the electron transport chain of Mycobacterium tuberculosis Andrew M. Thompson and William A. Denny 5. Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance Nicolas Willand, Marion Flipo, Baptiste Villemagne, Alain Baulard and Benoit Deprez 6. Sustainable anti-trypanosomatid drugs: An aspirational goal for medicinal chemistry Maria Laura Bolognesi