Novel therapies for tuberculosis
Tuberculosis is a bacterial infection caused by Mycobacterium tuberculosis that mainly affects the lungs. Although the disease can be treated with prolonged use of antibiotics, the emergence of drug resistance hampers bacterial eradication. As a result, novel, more specific drugs are urgently needed. The scope of the EU-funded TBKO (Synthesis and biological evaluation of a potent antituberculosis natural product and analogues) project was to synthesise and deliver natural-based products with anti-mycobacterial properties. In this context, their efforts focused on the characterisation and synthesis of the family of epidithiodiketopiperazines for tuberculosis treatment. During the TBKO project, a multiple-step procedure was developed, optimised and applied towards the synthesis of the parent compound. The synthesised products underwent biological evaluation, revealing important information about their structure. Researchers observed no significant activity against tuberculosis in its non-replicating form, but both compounds inhibited tuberculosis in its replicating form. This suggests a broader cytotoxicity and offers a better understanding of the mode of action of the family of epidithiodiketopiperazines. Considering the millions of tuberculosis-affected individuals worldwide and the need for effective treatments, TBKO deliverables open up opportunities for new antituberculosis drugs.