DESIGN OF MEDICINAL AKTIVE COMPOUNDS

ECZ436

Course Code: ECZ436
Semester: -
Theory+Practice: 2 + 0
ECTS: 2

Course Type

Elective Course

Course Level

Bachelor's Degree

Year of Study

Semester

ECTS

Name of Lecturer(s)

Professor Selma Saraç Tarhan

Learning Outcomes

At the end of this course, the students;

Stages of drug design and development and reasons for failure in drug development
Finding and optimizing the precursor compound
Molecular modification, bioisosterism, latent drug design, QSAR and QSAR parameters, combinatorial chemistry and rapid activity screening methods
Computer aided drug design
Have knowledge of drug repositioning and patents in medicine

Mode of Delivery

Face to face

Prerequisites

Recommended Optional Programme Components

None

Course Description

Fields of study of pharmaceutical and medicinal chemistry, historical development of drug discovery and development, stages of drug action, drug design and development stages, precursor compound discovery and optimization (molecular modification, rational drug design, latent drug design, QSAR), rational drug design and rational drug Examples of drugs developed with the design of drugs, computer aided drug design (structure and ligand-based drug design, bioinformatics, cheminformatics), purpose of drug repositioning and examples of repositioned drugs), patenting of drug active ingredient.

Course Contents

WEEK	TOPICS
1^st Week	INTRODUCTION: What is an active pharmacetical ingredient? The fields of pharmaceutical and medicinal chemistry?, Why do we use medicine? Historical evolution of drug discovery/drug development, Stages of drug action, Stages of drug development, reasons for the failure in drug development
2^nd Week	Drug design and development stages / Finding of a lead compound
3^rd Week	Finding of a lead compound: Rational drug design
4^th Week	Examples of drugs developed with rational drug design: Cimetidine and captopril
5^th Week	Drug design and development stages (continued) / Lead optimization: Molecular modifications and bioisosterism
6^th Week	Drug design and development stages (continued) / Lead optimization: Drug latentiation
7^th Week	Drug design and development stages (continued) / Lead optimization: Quantitative Structure Activity Relationships (QSAR)
8^th Week	Midterm exam
9^th Week	Combinatorial chemistry and High-Throughput Screening (HTS)
10^th Week	Computer Aided Drug Design (CADD)
11^th Week	Cheminformatic, bioinformatic (Protein Data Bank, PDB)
12^th Week	Problems and new approaches in drug development
13^th Week	Drug repositioning
14^th Week	Drug patents

Recommended or Required Reading

1. 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).

Planned Learning Activities and Teaching Methods

Lecture
Questions/Answers
Problem Solving
Discussion

Assessment Methods and Criteria

	Quantity	Percentage (%)
Mid-term	1	40
Total(%)		40
Contribution of In-term Studies to Overall Grade(%)		40
Contribution of Final Examination to Overall Grade(%)		60
Total(%)		100

ECTS Allocated Based on Student Workload

Activities	Quantity	Duration (Hour)	Total Workload (Hour)
Midterm exam	1	1	1
Preparation for Quiz	0	0	0
Individual or group work	14	1	14
Preparation for Final exam	1	10	10
Course hours	14	2	28
Preparation for Midterm exam	1	5	5
Laboratory (including preparation)	0	0	0
Final exam	1	2	2
Homework	0	0	0
Total Work Load			60
Total Work Load / 30 (h)			2
ECTS Credit of the Course			2

Language of Instruction

Turkish

Work Placement(s)

Programme Qualifications / Learning Outcomes

	LO1	LO2	LO3	LO4	LO5
K1
K2
K3
K4
K5	X	X	X	X	X
K6
K7					X
K8
K9
K10
K11
K12
K13
K14
K15				X
K16				X

	LO1	LO2	LO3	LO4	LO5
K1
K2
K3
K4
K5	X	X	X	X	X
K6
K7					X
K8
K9
K10
K11
K12
K13
K14
K15				X
K16				X

	LO1	LO2	LO3	LO4	LO5
K1
K2
K3
K4
K5	X	X	X	X	X
K6
K7					X
K8
K9
K10
K11
K12
K13
K14
K15				X
K16				X

	LO1	LO2	LO3	LO4	LO5
K1
K2
K3
K4
K5	X	X	X	X	X
K6
K7					X
K8
K9
K10
K11
K12
K13
K14
K15				X
K16				X