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Medicinal Chemistry (UAMC)
Main organisation:Department of Pharmaceutical Sciences
Lifecycle:1 Oct 2003 → Today
Organisation profile:The research topics in the Department of Medicinal Chemistry deal with the development of new medicines and focus mainly on following topics: 1. The investigation of enzymes as target for the design of biologically active compounds. Making use of the substrate selectivity of the enzyme, inhibitors are developed. Various medicinal chemical strategies and 'in silico' chemistry are used. These inhibitors are synthetized and chemically characterized. Solid phase chemistry and parallel synthesis procedures are used. New synthetic procedures are developed when necessary. After biochemical investigation, a structure-activity relationship is elaborated and inhibitors are optimized. Finally, the enzyme is evaluated as therapeutic target. Following inhibitor-enzym systems are being investigated: - Serine proteases of the SC clan: DPPII, DPPIV, DPP8, POP. - Urokinase plasminogen activator. - Parasitic cysteine proteases as falcipaïne and cruzipaïne. - Nucleoside hydrolase. - Nucleoside type inhibitors of viral enzymes. - Trypanothion synthetase. 2. Validation of natural compounds as potential medicine. From plants isolated biologically active compounds are optimized and a structure-activity relationship is elaborated. Actual research is dealing with cryptolepine alkaloids with antiplasmodial activity. 3. The development of new medicinal chemical strategies. The design of peptide mimicking scaffolds and the introduction of suitable side chains to investigate the peptide-receptor interaction and to develop non-peptide drugs. Priority is given to drug development in the field of tropical parasitic diseases.
Keywords:DRUG DESIGN, MEDICINAL CHEMISTRY, ORGANIC SYNTHESIS, NON-PEPTIDE DRUGS, TROPICAL DISEASE, PEPTIDASE, ONCOLOGY, INFECTIONS
Disciplines:Organic chemistry, Biomarker discovery and evaluation, Drug discovery and development, Medicinal products, Pharmaceutics, Pharmacognosy and phytochemistry, Pharmacology, Pharmacotherapy, Toxicology and toxinology, Other pharmaceutical sciences