SLVKM0381U Advances in Medicinal Chemistry Research

Volume 2013/2014
Education
MSc in Pharmaceutical Sciences - compulsory, MSc in Medicinal Chemistry - elective, Cand.Scient.Pharm. - elective, Cand.Pharm. - elective
Content
The course will be based on 3-4 major themes covering the objectives of the course. Hence, all subjects will be introduced in a theme driven interdisciplinary fashion. The themes will be illustrated by original scientific reports and may cover:
  • Target classes: receptors, transporters, enzymes, regulatory proteins
  • Target-ligand interactions
  • Structure – activity relationship (SAR) studies
  • Structure and ligand based drug design
  • Point of action and the prodrug concept
  • Peptidomimetics and protein based drugs
  • Drugability of lead compounds
  • Experimental methods in biological and biostructural chemistry
  • Basic and advanced medicinal chemistry concepts
  • 3D modeling of protein structure and ligand docking
As the course aims to highlight recent cutting edge research in medicinal/biostructural chemistry, themes vary but may cover: hypnotics, psychotropic drugs, immunomodulating agents, antiviral agents, neurotransmitters, chemotherapeutics, antineoplastics, drugs against neurodegenerative diseases and schizophrenia. During the course the students will cover three themes in groups of 4-5 persons. for each theme the groups will carry out literature search, write up a report and prepare a poster for oral presentation.

Beskrivelse af prøven og bedømmelse / Description of examination and assessment criteria

Prøvedesign / Examination design

Examination is based on a poster presentation, submitted by the student. To qualify for examination, the student must have submitted and approved written reports and participated in oral presentation of the subjects, based on poster presentations.
Learning Outcome
The original literature plays a pivotal role in the discovery of new drugs. In order to contribute to the process it is necessary to comprehend and to be able to communicate the content of primary research papers to others. The literature is the primary source of information in all steps of the drug discovery process including:
  • Biology of targets
  • Identification of interfering agents (drug candidates).
  • Optimization of interfering agents.
Importantly, the course aims at providing knowledge about the above-mentioned individual steps, while ensuring that the students do not consider each process isolated from the others. Hence, the students will have a collected understanding of biostructural/medicinal chemical aspects. Earlier courses provide in-depth insight to isolated techniques/theory. Rather, at this later time-point in the student’s education, an integrated view is acquired.
Drugs interfere with complex biological systems. In order to design targeted and specific drugs it is necessary to understand the system they interact with. Researchers will need to be able to quickly understand new techniques for the identification and optimization of biologics and small molecule compounds. The course objective is to train the students in acquiring the above-mentioned skills. They will work with original literature concerning particular indications. The indications may vary, and can include: cancer, diseases of the central nervous system, viral infections, neurodegenerative diseases, amyloid diseases.

At the end of the course, students will be able to:

  • Understand that particular cellular processes at the molecular level may lead to disease.
  • Understand and present the content of original literature describing complex biological systems of relevance in drug research.
  • Understand how the 3-dimensional structure of biological macromolecules plays a role for understanding the molecular basis of particular diseases, and for intervening with the disease progress.
  • Understand and present the content of original literature describing the identification of small molecule compounds that can interfere with complex biological systems.
  • Understand and present the content of original literature describing the optimization of small molecule compounds that can interfere with complex biological systems.
  • Understand and present the content of original literature describing the impact of interfering with protein-protein interactions using designed biological macromolecules (biologics).
Literature
Reviews and original scientific papers available at the course website
The teaching is arranged with the assumption that students have knowledge from basal courses in organic chemistry, physical chemistry, biochemistry, general pharmacology and medicinal chemistry.
•Lectures: 9
•Class lessons: 17
  • Category
  • Hours
  • Exam
  • 0,5
  • Lectures
  • 26
  • Preparation
  • 91,5
  • Project work
  • 88
  • Total
  • 206,0
Credit
7,5 ECTS
Type of assessment
Oral examination
Examination is based on a poster presentation, submitted by the student.
The exam is without preparation time.
Exam registration requirements
To qualify for examination, the student must have submitted and approved written reports and participated in oral presentation of the subjects, based on poster presentations.
Aid
Only certain aids allowed
None, except the poster presentation, which is drawn as the exam subject.
Marking scale
7-point grading scale
Censorship form
No external censorship
Criteria for exam assesment
12 - Excellent performance
A comprehensive collected understanding and knowledge of biostructural/​medicinal-chemical aspects in the drug discovery process. The student demonstrates the ability to understand and present the content of original literature describing:
  • complex biological systems of relevance in drug research.
  • identification of small molecule compounds that can interfere with complex biological systems.
  • optimization of small molecule compounds that can interfere with complex biological systems.
  • the impact of interfering with protein-protein interactions using designed biological macromolecules.
7 - Good performance
A reasonable level of understanding and knowledge of biostructural/​medicinal-chemical aspects in the drug discovery process. The student demonstrates in general with some weaknesses the ability to understand and present the content of original literature describing:
  • complex biological systems of relevance in drug research.
  • identification of small molecule compounds that can interfere with complex biological systems.
  • optimization of small molecule compounds that can interfere with complex biological systems.
  • the impact of interfering with protein-protein interactions using designed biological macromolecules.
02 - Acceptable performance
A reasonable level of understanding and knowledge of biostructural/​medicinal-chemical aspects in the drug discovery process. The student demonstrates in general with several weaknesses the ability to understand and present the content of original literature describing:
  • complex biological systems of relevance in drug research.
  • identification of small molecule compounds that can interfere with complex biological systems.
  • optimization of small molecule compounds that can interfere with complex biological systems.
  • the impact of interfering with protein-protein interactions using designed biological macromolecules.