KE828: Medicinal chemistry B

Study Board of Science

Teaching language: Danish or English depending on the teacher, but English if international students are enrolled
EKA: N540040102, N540040112
Assessment: Second examiner: External, Second examiner: None
Grading: 7-point grading scale, Pass/Fail
Offered in: Odense
Offered in: Spring
Level: Master

STADS ID (UVA): N540040101
ECTS value: 5

Date of Approval: 31-10-2022


Duration: 1 semester

Version: Archive

Comment


Entry requirements

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.

Content

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

See itslearning for syllabus lists and additional literature references.

Examination regulations

Exam element a)

Timing

June

Prerequisites

Type Prerequisite name Prerequisite course
Examination part Prerequisites for participating in the exam a) N540040101, KE828: Medicinal chemistry B

Tests

Oral examination

EKA

N540040102

Assessment

Second examiner: External

Grading

7-point grading scale

Identification

Student Identification Card

Language

Normally, the same as teaching language

Duration

25 minutes

Examination aids

Article, presentation (for instance PowerPoint), and computer for the presentation. 

ECTS value

5

Additional information

Oral examination without preparation time. Article for the exam will be handed out no later than two weeks before the exam.

Prerequisites for participating in the exam a)

Timing

Spring

Tests

4 electronic tests

EKA

N540040112

Assessment

Second examiner: None

Grading

Pass/Fail

Identification

Full name and SDU username

Language

Normally, the same as teaching language

Examination aids

To be announced during the course.

ECTS value

0

Additional information

The prerequisite examination is a prerequisite for participation in exam element a)

Indicative number of lessons

42 hours per semester

Teaching Method

At the faculty of science, teaching is organized after the three-phase model ie. intro, training and study phase.
  • Intro phase - 26 hours
  • Training phase: 16 hours, including 16 hours tutorials
Activities during the study phase:
  • Self-study of course book and articles
  • Solve exercises
  • E-tests
  • Preparation of student presentations
  • Revision for the exam

Teacher responsible

Name E-mail Department
Jasmin Mecinovic mecinovic@sdu.dk Institut for Fysik, Kemi og Farmaci

Timetable

Administrative Unit

Fysik, kemi og Farmaci

Team at Educational Law & Registration

NAT

Offered in

Odense

Recommended course of study

Transition rules

Transitional arrangements describe how a course replaces another course when changes are made to the course of study. 
If a transitional arrangement has been made for a course, it will be stated in the list. 
See transitional arrangements for all courses at the Faculty of Science.