Lead Compound Diversification and C-H Activation
Our microbial panels not only mimic mammalian metabolism but have the added benefit of also producing other derivatives that might not have been considered or accessible using synthetic routes. The process is complementary to medicinal chemistry and can be exploited to diversify hit or lead compounds by generating oxidised molecules that may have greater activity, better selectivity or an improved availability profile than the parent molecule. It can also be used to help widen and protect IP and inform SAR. The technology can be applied at the lead optimisation stage or on compounds at earlier hit or hit-to-lead stages.
Solve Excessive Lipophilicity
If you are looking to create more polar metabolites to improve solubility, we can apply our proven lipophilic rescue service to achieve improvement in LLE/LipE. The technology has the added benefit that multiple analogues can be produced in a single process. Selected derivatives can then be optimised and the production scaled-up.
Create Handles for Synthesis
Our process can create handles for further structural changes such as fluorination used for metabolism blocking or PET ligand formation.
Key features of our lead diversification service:
- Flexible options – the process can be tailored to client needs
- Provides a unique method for generating metabolites that are challenging to create synthetically
- Scalable and reproducible process
- Multiple metabolites can be captured in a single screen
- Applicable to broad structural types and complex molecules, including natural products
- Target molecules are produced at mg/g scale
- Defined timelines and costs
- Metabolites are produced on a simple fee-for-service basis, i.e. there are no downstream terms
Download our poster on Microbial Hydroxylation of Lead Compounds: A Way Out of the Lipophilic Cul-de-Sac presented at the RICT Conference in France in 2014
Please contact us to discuss options.