Objectives

This is, from the discovery of an active molecule, to provide a consistent set of approaches and tools promoting chemical development. This organic synthesis offer is developed in synergy with the analysis and purification service already present on the Chemistry platform hosted by the SPCMIB laboratory.

The objective is to provide a chemical synthesis service fully integrated with the identification of ligands implemented programs within the Integrated Screening Platform of Toulouse (PICT), ISO 9001 certified member of GIS Genotoul and IBiSA and member of the national research infrastructure ChemBioFrance.

Description

Three types of services are offered:

Preparation of a synthetic ligand of interest that is not very accessible: a commercial or published molecule is unavailable or inaccessible. The service consists in synthesizing the compound in order to deliver an agreed quantity and / or in developing a transferable multi-stage synthesis pathway.
- Exploration of the chemical space around an active molecular scaffold: new chemotypes call for additional studies. The service relates to the resynthesis of the hit and the synthesis of a defined number of close derivatives by post-functionalization or synthesis in series.
- Exploitation of fragments identified by screening: one or more active fragments are selected to construct a molecule of greater size and affinity. The service concerns the generation of a defined number of compounds inspired by the selected fragments.

Depending on the type of project, they can be conducted in the form of a simple or collaborative service.

Results

Deliverables are either items of synthesized compounds (of about ten mg to several g), or the description of the expanded synthetic route, or both. The batches of compounds prepared will be accompanied by reports describing the analysis results which have made it possible to identify and determine the purity of the molecule by the usual spectroscopic techniques in organic synthesis. The state of purity and quantity will comply with what has been previously defined in the quotation. The description of the synthetic routes developed will also be provided in the form of a report detailing for each step the reaction processes and the characterizations of the intermediate compounds.

Outlook

Ultimately, these services will be extended to the in-depth optimization of keys from the screening of chemical libraries for which:

- the activity and physico-chemical profiles must be improved and / or
- the mechanism of action must be probed using dedicated molecular tools.

These activities could be developed within the framework of a research partnership.