EFK736 - BASIC PRINCIPLES IN DRUG DESIGN II

Course Name Code Semester Theory
(hours/week)		 Application
(hours/week)		 Credit ECTS
BASIC PRINCIPLES IN DRUG DESIGN II EFK736 3rd Semester 2 0 2 7
PrequisitesBeing successful in EFK 635 Basic Principles in Drug Design I
Course languageTurkish
Course typeMust 
Mode of DeliveryFace-to-Face 
Learning and teaching strategiesLecture
Problem Solving
 
Instructor (s)Prof. Dr. Birsen Tozkoparan Köprücü, Doç. Dr. Miyase Gözde Gündüz 
Course objectiveInteractions between drug molecules and organism, classification of drugs, rational drug design and overview of computer aided drug design, QSAR parameters and case studies for QSAR, the role of combinatorial chemistry in drug design, pre-clinical ana clinical trials, basic concepts of drug registration. 
Learning outcomes
  1. The student who completes this course learn:
  2. 1. Pharmacokinetic principles important for new drug design and development,
  3. 2. Prodrug concept and its importance in drug development,
  4. 3. QSAR and parameters used in QSAR studies for drug development,
  5. 4. Rational drug design and overview for computer aided drug design and combinatorial chemistry,
  6. 5. Preclinical and clinical trials for drug development and drug registration studies.
Course ContentDrug activity and pharmacokinetic principles, drug latentization and prodrug approach, rational drug design and computer aided drug design, high throughput screening methods and combinatorial chemistry, quantitative structure activity relationships (QSAR) and QSAR parameters, planing of a QSAR study and case studies, preclinical and clinical trials in drug development and drug registration  
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., Şafak, C., Tozkoparan, B.: Farmasötik Kimya, 2. Baskı, Ankara (2004).
2. Patrick, G.L.: An Introduction to Medicinal Chemistry, Oxford University Press, Oxford (1999).
3. Korolkovas, A.: Essentials of Medicinal Chemistry, Wiley-Interscience, New York (1988).
4. King, F.D. (ed): Medicinal Chemistry: Principles and Practice, The Royal Society of Chemistry, Cambridge (1994).
5. Silvermann, R.D.: The Organic Chemistry of Drug Design and Drug Action, Academic Press, Oxford (1992).
6. Smith, H.J.: Smith and Williams? Introduction to the Principles of Drug Design, 2nd ed., Wrigth (1988).
7. Kayaalp, S.O.: Klinik Farmakolojinin Esasları ve İnsandaki İlaç Araştırmaları ile İlgili Resmi Düzenlemeler, Ankara ( 1996).
8. Wermuth, C.G.: The Practice of Medicinal Chemistry, London (2001). 

Course outline weekly

WeeksTopics
Week 1Classification of drugs (structure spesific and structure nonspesific drugs), drug and organism, pharmacokinetic principles
Week 2Pharmacokinetic principles
Week 3Drug latentization, prodrugs (carrier-prodrugs and bioprecursors), targeted drugs
Week 4Prodrug examples in the market
Week 5Rational drug design and case study
Week 6Methods used for rational drug design, computer aided drug design (ligand-based and structure based design)
Week 7Cheminformatic ana bioinformatic
Week 8Virtual screening
Week 9QSAR and QSAR parameters
Week 10Design and steps of a QSAR study, case studies
Week 11High throughput synthesis, combinatorial chemistry and high throughput activity screening methods
Week 12Preclinical trials
Week 13Clinical trials (Phase studies)
Week 14Registration of a drug and legal aspects
Week 15Presentation of an article and preparation to final exam
Week 16Final Exam

Assesment methods

Course activitiesNumberPercentage
Attendance00
Laboratory00
Application00
Field activities00
Specific practical training00
Assignments130
Presentation00
Project00
Seminar00
Midterms00
Final exam170
Total100
Percentage of semester activities contributing grade succes130
Percentage of final exam contributing grade succes170
Total100

WORKLOAD AND ECTS CALCULATION

Activities Number Duration (hour) Total Work Load
Course Duration (x14) 14 2 28
Laboratory 0 0 0
Application000
Specific practical training000
Field activities000
Study Hours Out of Class (Preliminary work, reinforcement, ect)14684
Presentation / Seminar Preparation000
Project000
Homework assignment15050
Midterms (Study duration)000
Final Exam (Study duration) 14848
Total Workload30106210

Matrix Of The Course Learning Outcomes Versus Program Outcomes

D.9. Key Learning OutcomesContrubition level*
12345
1. Able to make a research plan related to their study subject and workspace.   X 
2. Presents study findings at scientific conferences and converts them into articles.X    
3. Has sufficient knowledge about scientific ethic and ethical principles for experiments on human and animals.   X 
4. Makes literature search based on subject title.     
5. Develops novel molecules and synthesis methods based on the information obtained.   X 
6. Uses technology to follow scientific innovations and to reach desired information.  X  
7. Synthesizes designed molecules by obeying the rules of laboratory safety.     
8. Has the required knowledge and skills on experimental designs and using instrumental analysis devices.     
9. Creates solutions on acute problems during synthetic and analytical studies. X   
10. Capable of planning, writing and managing and evaluating other projects.X    
11. Plans a multidisciplinary study and arranges coordination between study groups.     
12. Has knowledge of one foreign language, enabling written and oral communication.  X  
13. Attends national and international symposiums to stay updated on developments.     
14. Enhances professional knowledge and remains open to developments.  X  
15. Interprets instrumental data to formulate predictions and arrives at appropriate solutions. X   

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