After this course, the student is able to:
- explain the effect as well as the fate of drugs in the human body from the point of view of molecular targets and mode of action
- understand and apply the techniques and methods of pharmacochemistry that are operative in the development of new drugs
- describe the relationship between structure and activity of drugs both in a qualitative and quantitative manner.
Pharmocochemistry (medicinal chemistry) comprises a multidisciplinairy field that focuses on the relationship between chemical structure and biological activity of drugs at a molecular level. An important target of pharmacochemistry is the development of new drugs and other biologically active substances. In order to develop a new drug, medicinal chemists are involved in the design, organic synthesis, structural elucidation and pharmacological-toxicological research of biologically active compounds.
This course will discuss the fundamental principles underlying the mode of action and metabolism of drugs in the human body. Apart from that, an overview will be provided of the specific methods applicable for design, synthesis and optimization of new drugs, with particular focus on the relationship between structure and activity. Topics that will be discussed:
- drug development process - role of pharmacochemistry
- receptor pharmacology
- dose-response relationships
- absorption, distribution, biotransformation, excretion and toxicity
- molecular design strategies
- (quantitative) structure-activity relationships
- computer-assisted drug design
- combinatorial chemistry
- drugs acting on the nervous system
- antibiotics and cytostatics