Novel antibiotics by rational drug design
The discovery of new antibiotic drugs is based on the isolation of compounds that are screened for bacteriocidal or bacteriostatic activity. These compounds may either be chemically synthesised or isolated from nature. An additional route to drug discovery is rational drug design.
Protein structural analysis, active site modification and reaction mechanism studies performed at the CSIR have identified an enzyme as a potential new drug target for the disease. Structural analysis of reaction intermediates has identified novel molecules as potential drug candidates with application to tuberculosis, as well as other bacterially induced diseases.
The innovative research and development phase of the project will comprise further structural analysis and molecular modelling of the drug candidates and enzyme, synthesis of the potential drug analogs followed by in vitro enzymatic analysis of efficacy. An analysis of efficacy against growth and the infection process of the pathogen responsible for the disease (Mycobacterium tuberculosis) will also be undertaken.
This project is being undertaken in collaboration with a number of partners in South Africa, with funding from the Innovation Fund.