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Medicinal Chemistry Services

By Syncom BV pbr

Syncom's services as an integrated drug discovery contract research organisation (CRO), includes synthetic chemistry, in vitro screening, ADME studies, pharmacokinetics and in vivo pharmacology.

syncom-medicinal-chemistry

Hit finding and library preparation

For hit finding, Syncom has access to a novel fragment-based library (>1500 compounds), applying the rule of three and a novel drug-like library (1200 compounds, in progress).

Syncom has successfully performed several screening campaigns, including in-house assay development. We also have excellent relationships with several European (high-throughput) screening facilities and expertise with assay development for HTS screening.

Syncom has up-to-date facilities for preparation of focused libraries in-line with properties requested (drug-likeness and preferably logP (D) < 5, Mwt < 500). We have more than 10,000 scaffolds and decorating agents (amines, carboxylic acids, aldehydes, boronic acids, etc.) on the shelf available for immediate use.

Our set of scaffolds includes unique compounds, sp3-rich scaffolds and compounds having multiple points for further decoration. Furthermore, we are highly experienced in the preparation of (diverse) libraries based upon multicomponent reactions (MCR) and secondary transformations thereof.

Hit to lead

Validated chemical classes will be selected for further hit appraisal. The prioritisation will be based upon the initial potency and physical parameters. Undesirable features will be identified (chemical instability, dependence on a toxicophore, metabolic vulnerabilities) and excluded upfront. Depending on the desires of our clients, Syncom can include computational advice from leading CROs in this field and design the compounds to be synthesised based upon criteria described above.

In general our synthetic program will attempt to improve the on-target activity, while simultaneously balancing physical parameters, such as solubility, lipophilicity, permeability and metabolic stability. Classes of compounds will be progressed to proof of concept in vivo efficacy. We also successfully participated in hit-to-lead programs for so-called multiple ligands (molecules active on several targets), resulting in two patent applications.

Lead optimisation

Lead optimisation at Syncom is generally performed with our preferred partners, Brains-on-Line and Integrex Research. Through an iterative process, we optimise pharmacokinetic and in vivo pharmacology results obtained, ultimately leading to a pre-clincial candidate.

Our long-standing collaboration with our partners, enables fast and effective communication and shortens the lead optimisation phase significantly.

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