270193 VO Pharmaceutical and solution chemistry of (metallo)drugs (2020S)
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Language: English
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All lectures will take place in lecture room 4, Währinger Straße 42, Halbstock. 03.06., 10.00-12.00, 04.06., 14.00-16.00, 16.06. 10.00-12.00, 17.06., 10.00-12.00, 23.06., 10.00-12.00, 24.06., 10.00-12.00, 25.06., 10.00-12.00, 30.06., 10.00-12.00
Information
Aims, contents and method of the course
Assessment and permitted materials
Minimum requirements and assessment criteria
Examination topics
Reading list
Medicinal Chemistry: Principles and Practice (Ed. F.D. King), Royal Society of Chemistry, 2002.; M.T. Beck; I. Nagypál; Chemistry of Complex Equilibria, Ellis Horwood, Chichester, UK, 1990; Metallotherapeutic Drugs and Metal-based Diagnostic Agents (Eds, M. Gielen, E.R.T. Tiekink), Wiley, Chichester, 2005.
Association in the course directory
EF-1, EF-2, EF-3
Last modified: We 19.08.2020 07:49
Factors affecting pharmacokinetics (LADME properties: liberation, absorption, distribution, metabolism, excretion), bioavailability, accumulation, biofluids; routes of drug administration. Acid-base properties: macroconstants and microscopic proton dissociation constants. Lipophilicity, solubility and their modifications. Experimental determination of pKa and logP values. Biological pH-buffers.
Metal containing drugs (anticancer/-bacterial/-diabetic; chelate therapy). Solution stability of metal complexes, complex formation equilibrium processes. Conditional stability constants. Concentration distribution. Experimental determination of stability constants. Lipophilicity of metal complexes. Redox properties of metal complexes.
Prodrugs (metallic, nonmetallic).
Effect of interaction with biological macromolecules (proteins, DNA) on pharmacokinetics. Plasma protein binding. Experimental determination of binding sites and binding constants of protein-ligand adducts.