Medicinal Chemistry

Medicinal chemistry is our core expertise. With our experience of dealing with several different targets and dealing with various novel chemotypes, we can support your team, we can be your team or we can manage your program. We can creatively solve various issues facing drug discovery, we can effectively collaborate with biology, DMPK group using either our internal resources or working with your internal groups.

• Prioritizing hits form High throughput screening
• Resynthesis of hits as well as close analogs and confirming biological activity
• Hit to lead – establishing early SAR
• Lead optimization – drug like properties, addressing potency issues, addressing pK issues as well as toxicological related issues.
• Structure based drug design

Synthetic Chemistry

• Synthesis of key intermediates, reference compounds, process impurities and scale up for in vivo experiments

Structure Characterization and Identification

• • With our expertise in NMR methods, as well as using our own MS/MS method, we can help to solve any structural characterization problems.

Pharmaceutical Suitability Characterization (In vitro)

• Stability - Light
• Stability – Heat
• Stability in simulated gastric conditions (for oral drugs)
• Permeability CaCo cells
• Blood/Plasma stability
• Plasma protein binding (free fraction)
• Metabolic Stability (S9, Microsomes)
• Liver Enzyme Inhibition
• Metabolite Identification

Pharmacokinetic Evaluation (In-vivo)

• Oral PK (rats, mice)
• Bioavailability