KE828: Medicinal chemistry B (5 ECTS)

STADS: 10010701

Level
Master's level course

Teaching period
The course is offered in the autumn semester.

Teacher responsible
Email: elc@sdu.dk

Timetable
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Prerequisites:
A Bachelor’s degree in chemistry or pharmacy.

Academic preconditions:
Students taking the course are expected to:

• Have knowledge of basic biochemistry
• Have knowledge of fundamental organic chemistry
• Have knowledge of fundamental medicinal chemistry

Course introduction
The aim of the course is to enable the student to understand the effect of physico-chemical properties of a drug on the pharmacokinetic properties and how to optimize these, which is important in regard to development of new drugs with good ADMET properties.

The course builds on the knowledge acquired in the courses medicinal chemistry A (KE511/FA506), organic chemistry (KE505) and basic biochemistry (BMB530), and gives an academic basis for performing a master thesis within the field of medicinal chemistry.

In relation to the competence profile of the degree it is the explicit focus of the course to:

• Give the competence to take responsibility for own  professional development
• Give the competence to development solution models both individually and in teams across study background (chemistry/medicinal chemistry/pharmacy)
• Give skills to communicate and critically analyse research results and research-based knowledge
• Give knowledge and understanding of important elements in drug design and optimization in the pre-clinical phase of drug development
• Give knowledge and understanding of experimental methods used within medicinal chemistry research

Expected learning outcome
The learning objectives of the course are that the student demonstrates the ability to:

• Explain the effect of physico-chemical properties on drugs ADMET properties.
• Explain and discuss different optimization strategies of physico-chemical properties including the use of physico-chemical decriptors.
• Explain target-ligand interactions and methods for optimization of these.
• Discuss medicinal chemistry articles containing ADMET data.

Subject overview
The following main topics are contained in the course:

• Physicochemical properties and descriptors (pKa, lipophilicity, solubility, Fsp³, LE, LLE etc.)
• ADMET (permeability, metabolic stability, plasma stability, CYP inhibition, hERG blocking, toxicity, pharmacokinetics, blood-brain barrier)
• Optimization strategies (e.g. the use of fluorine and deuterium)
• Target-ligand interactions
• Fragment based drug design
• Modeling in medicinal chemistry (pharmacophores, homology models, docking, in silico screening)
• Case studies

Literature
There isn't any litterature for the course at the moment.

Website
This course uses e-learn (blackboard).

Prerequisites for participating in the exam

1. 4 electronic tests. Internal evaluation by teacher, pass/fail. (10010712).

Assessment and marking:

1. Oral examination without preparation time, external marking, Danish 7-mark scale. Article for the exam will be handed out no later than two weeks before the exam. Allowed exam aids: Article, presentation (for instance PowerPoint), and computer for the presentation. (5 ECTS). (10010702).

Expected working hours
The teaching method is based on three phase model.
Intro phase: 26 hours
Skills training phase: 16 hours, hereof:
 - Tutorials: 16 hours

Educational activities

Educational form
Activities during the study phase:

• Self-study of course book and articles
• Solve exercises
• E-tests
• Preparation of student presentations
• Revision for the exam

Language
This course is taught in Danish or English, depending on the lecturer. However, if international students participate, the teaching language will always be English.

Course enrollment
See deadline of enrolment.

Tuition fees for single courses
See fees for single courses.