CloseHelpPrint
Kies de Nederlandse taal
Course module: UCSCICHE32
UCSCICHE32
Medicinal Chemistry
Course info
Course codeUCSCICHE32
EC7.5
Course goals
After completing this course, students are able to:
  • Recall the basic methodologies of drug discovery, including target discovery, lead compound identification and understand the process of drug development with an emphasis on structure-activity relationships on a molecular level
  • Demonstrate insight into the chemical synthesis of biologically active compounds, based on selected examples, like Tamiflu, Maraviroc and antibiotics. 
Content
In Medicinal Chemistry, the chemist attempts to discover, design, and synthesize a pharmaceutical agent that has a desired biological effect on the human body. Drug discovery and design involves a multidisciplinary approach, where the established disciplines medicine, biology, chemistry and pharmacy have sprouted new methodologies for target discovery, lead discovery, lead characterization and optimization, and lead compound synthesis. This course introduces methods and approaches that are currently used in medicinal chemistry with an emphasis on molecular interactions and chemical synthesis of drugs and drug-like compounds.
After a short introduction on general chemical properties of molecules, the course starts with describing the appropriate targets for drug design: receptor proteins and enzymes. To be active as a drug, the physicochemical properties of the compound that are important for activity, like absorption, distribution, metabolism and elimination, are defined and discussed. Lead compounds are subjected to several routes for optimization such as combinatorial chemistry, quantitative structure activity relationships, molecular mechanics and dynamics, and high throughput screening. Given a biologically active compound, the chemical synthesis and issues with respect to process development are discussed. Most examples will be taken from antibacterial and antiviral drug discovery and design processes, including considerations with respect to drug targeting and delivery, toxicity and the emerging problem of drug resistance.

 
Format
The course will be given by twolecturers. Students and lecturer come together during four hours/week. These meetings consist of three elements:
  • Lectures and tutorials: the lecturer discusses the topic illustrated with examples from the current literature and will explain the basic principles of drug development in relation to the chosen topic. In the intervening period, the students are expected to study the relevant chapter(s) or primary literature for the next session.
  • Workshops: these sessions illustrate the students computational and theoretical aspects of drug design and discovery.
  • Preparation of a written report that deals with drug design and development.
  • Preparation of a drug monograph: each individual student prepares an oral presentation about ‘the birth and life of a first-in-class drug’, in which the following topics should be addressed: the history of its discovery, basic aspects of its chemical synthesis, the disease it treats, and its physicochemical and pharmacokinetic/dynamic properties. The content of the presentation will be discussed with lecturer and the students.
Workshops: these sessions illustrate the students computational and theoretical aspects of drug design and discovery.
Preparation of a written report that deals with drug design and development.
Preparation of a drug monograph: each individual student prepares an oral presentation about ‘the birth and life of a first-in-class drug’, in which the following topics should be addressed: the history of its discovery , basic aspects of its chemical synthesis, the disease it treats, and its physicochemical and pharmacokinetic/dynamic properties. The content of the presentation will be discussed with lecturer and the students.
 
CloseHelpPrint
Kies de Nederlandse taal