EAG602 - BASIC PRINCIPLES IN MEDICINAL CHEMISTRY

Course Name Code Semester Theory
(hours/week)		 Application
(hours/week)		 Credit ECTS
BASIC PRINCIPLES IN MEDICINAL CHEMISTRY EAG602 2nd Semester 3 0 3 5
Prequisites
Course languageTurkish
Course typeMust 
Mode of DeliveryFace-to-Face 
Learning and teaching strategiesLecture
Discussion
Problem Solving
 
Instructor (s)Prof. Dr. Nesrin Gökhan Kelekçi, Prof. Dr. Birsen Tozkoparan Köprücü 
Course objectiveThe purpose of this course is to give basic theoretical knowledge on description and history of pharmaceutical and medicinal chemistry, the effects of the physicochemical and structural properties on the activity, drug-receptor interactions, drug metabolism reactions and their importance in drug development. 
Learning outcomes
  1. History and description of pharmaceutical chemistry.
  2. The effects of the physicochemical and structural properties on the activity, drug-receptor interactions, drug metabolism reactions and their importance in drug development
Course Content-General principles, classifications, syhtheses, structure-activity relationships and metabolism of central nervous system and analgesic drugs. 
References1. Akgün, H., Balkan, A., Bilgin, A.A., Çalış, Ü.,Dalkara, S., Erdoğan, H., Erol Demir, D., Ertan, M.,Gökhan, N., Özkanlı, F., Palaska, E., Saraç, S. ve Şafak, C.,Tozkoparan.B.: FarmasötikKimya, Ankara, 2004.
2. Foye, W.O.(ed): Principles of Medicinal Chemistry, 3rd ed, Lea &Febrigen, Philadelphia, 1989.
3. Delgado, J.N., Remers, W.A. (ed), Wilson &Gisvold?s Textbook of Organic Medicinal and Pharmaceutical Chemistry, 9th ed., Lippincott, Philadelphia, 1991.
4. Patrick, G.L., An Introduction to Medicinal Chemistry, Oxford University Press, Oxford, 1999. 

Course outline weekly

WeeksTopics
Week 1Introduction to pharmaceutical-medicinal chemistry, principles, history, types of active drugs
Week 2Drug and organism: Pharmacokinetic principles
Week 3Receptors and drug-receptor interactions: Bonds, stereoselectivity, drug-receptor interaction teories
Week 4Structure-activity relationships: Physicochemical properties and drug activity; solubility, partition coefficient
Week 5Structure-activity relationships: Physicochemical properties and drug activity, surface activity, ionisation
Week 6Structure-activity relationships: General properties of fontional groups in drugs, isomerism, bioisomerism, steric parameters, molecular connectivity index, pharmacological effects of specific groups
Week 7Qualitative structure-activity relationships: Methods available: common methods used to correlate with physicochemical properties and biological activity
Week 8Drug metabolism: Structure of drug and metabolism, metabolism pathways, Phase I and II reactions
Week 9Midterm exam
Week 10Drug metabolism: Drug metabolism studies, effects of drug metabolism on drug activity and its importance in drug development
Week 11Drug design and development: Development pathways, discovery and optimisation of lead drug
Week 12Drug design and development: Development pathways, latent drug(prodrug and its requirement, targeted drug), softdrug, combinatorial chemistry
Week 13Current methods in active ligand design, ligand based drug development methods (QSAR, pharmacophore analysis)
Week 14Current methods in active ligand design, structure based drug development methods (Docking, De novo, Virtual screening and 3D visualization)
Week 15Recovery
Week 16Final exam

Assesment methods

Course activitiesNumberPercentage
Attendance00
Laboratory00
Application00
Field activities00
Specific practical training00
Assignments00
Presentation00
Project00
Seminar00
Midterms150
Final exam150
Total100
Percentage of semester activities contributing grade succes150
Percentage of final exam contributing grade succes150
Total100

WORKLOAD AND ECTS CALCULATION

Activities Number Duration (hour) Total Work Load
Course Duration (x14) 14 3 42
Laboratory 0 0 0
Application000
Specific practical training000
Field activities000
Study Hours Out of Class (Preliminary work, reinforcement, ect)14570
Presentation / Seminar Preparation000
Project000
Homework assignment000
Midterms (Study duration)11515
Final Exam (Study duration) 12323
Total Workload3046150

Matrix Of The Course Learning Outcomes Versus Program Outcomes

D.9. Key Learning OutcomesContrubition level*
12345
1. Has knowledge in the area of preformulation and formulation designs about industrial production, quality control, quality assurance system and stabilityX    
2. Acquires information about nanotechnology, new drug delivery systems and controlled release systems  X  
3. Learns to keep track of up to date literature and patents using the knowledge and informatics technologies  X  
4. Interprets the guidelines of health authorities such as FDA, EMA and international guidelines such as GMP, ANDA, BA/BE, QA/QC, acquires application knowledge and skills     
5. Has knowledge to understand and interpret chemical, instrumental and pharmacological data X   
6. Has basic concepts about medicinal chemistry such as design of new drug molecules, drug-receptor interactions   X 
7. Has the knowledge on the rules of scientific ethics which should be compliedX    
8. Effectively uses the conventional and new synthetic methods.X    
9. Has knowledge of advanced toxicity tests accepted by regulatory authorities     
10. Has knowledge about pharmacological experimental methods and their applications used in drug research and evaluates analysis results     
11. Has knowledge about preclinical and clinical drug research     
12. Has knowledge about the pharmacokinetic and pharmacodynamic properties of drugs  X  
13. Has knowledge about the pharmacokinetics and pharmacodynamics of drugs     
14. Has knowledge of and the ability to use the devices and instruments used in the application of instrumental analysis methodsX    
15. Has the ability to apply theoretical and practical knowledge in the analysis of substances in medicinal products and biological materials     

*1 Lowest, 2 Low, 3 Average, 4 High, 5 Highest