Working with our partners in the NABARSI consortium, Oxford Drug Design has discovered inhibitors of aaRS enzymes. Using our drug-design expertise, we have optimized these compounds to introduce antibacterial activity and developed a backup class of compounds. Our cheminformatics analysis of antibacterial molecules has helped guide us to the right area of chemical space to exhibit antibacterial activity. We continue to apply machine-learning techniques to gain a better understanding of antibacterial properties.
The two compound series have antibiotic activity against Gram-negative pathogens including several key ESKAPE organisms and resistant strains that are urgent and urgent and serious threats to public health. The compounds are not cross-resistant to existing classes of antibiotics, such as penicillins and fluoroquinolones and we are pursuing novel strategies to minimize the development of resistance, in order to improve clinical utility.
We are currently improving potency and spectrum of activity as we advance the compounds towards clinical candidate status.
This work is partly funded by Innovate UK, the UK's innovation agency, and previously by the European Union Framework Programme 7.
Further pre-clinical antibacterial projects focused on novel mechanisms of action and with potential human and veterinary applications complete the InhibOx pipeline of drug discovery projects. Applications to parasitic diseases and other therapeutic areas are also envisaged.