ECS518 Drug Active Ingredient Design

3 ECTS - 2-0 Duration (T+A)- 10. Semester- 2 National Credit

Information

Code ECS518
Name Drug Active Ingredient Design
Term 2024-2025 Academic Year
Semester 10. Semester
Duration (T+A) 2-0 (T-A) (17 Week)
ECTS 3 ECTS
National Credit 2 National Credit
Teaching Language Türkçe
Level Lisans Dersi
Type Normal
Mode of study Yüz Yüze Öğretim
Catalog Information Coordinator Dr. Öğr. Üyesi ÖZDEN TARI
Course Instructor
1 2
Dr. Öğr. Üyesi ÖZDEN TARI (A Group) (Ins. in Charge)


Course Goal / Objective

Understanding of approaches used for the design of drug molecules.

Course Content

Historical backround of drug design and discovery. Drug-receptor interactions and bond types involved in these interactions. The role of water/lipid solubility in binding, distribution and metabolism of drugs. The importance of stereochemistry in drug action, conformationla flexibility, rigid analogs. The importance of structure-activity relationships for new drug design and the role of acidity-basicity in drug effect. Approaches used for the definition of lead compound. Design based on target macromolecules, endogenous molecules, analogue design, combinatorial chemistry. Pharmacophore definition, lead compound modification and optimization .Bioisosterism, classical and non-classical bioisosters .Prediction of lipophilicity, ionization and steric parameters. Pro-drug design, drug targeting and soft drug design. Drug design based on enzymes, enzyme inhibitors. Toxic effects due to the functional groups and their correction Examples of succesful applications for rational drug design.

Course Precondition

None

Resources

H. Akgün, A. Balkan, A. A. Bilgin, Ü. Çalış ve ark. Farmasötik Kimya Kitabı, Hacettepe Üniversitesi Yayınları, 2013. SC Gad (Ed.), Drug discovery handbook, John Wiley and Sons, Inc., 2005. An Introduction to Medicinal Chemistry, Gareth Thomas, Wiley.

Notes

H. Akgün, A. Balkan, A. A. Bilgin, Ü. Çalış ve ark. Farmasötik Kimya Kitabı, Hacettepe Üniversitesi Yayınları, 2013. SC Gad (Ed.), Drug discovery handbook, John Wiley and Sons, Inc., 2005. An Introduction to Medicinal Chemistry, Gareth Thomas, Wiley.


Course Learning Outcomes

Order Course Learning Outcomes
LO01 The student who completes this course describes the basic concepts and principles of designing drug substances.
LO02 The student who completes this course evaluates the new developments in active substance design.
LO03 The student who completes this course makes literature researches on development of active drug substances.
LO04 The student who completes this course explains the approaches applied to drug design.
LO05 The student who completes this course develops model compounds by drug design.


Relation with Program Learning Outcome

Order Type Program Learning Outcomes Level
PLO01 Bilgi - Kuramsal, Olgusal Have sufficient knowledge in pharmaceutical field and develop the knowledge. 3
PLO02 Bilgi - Kuramsal, Olgusal Comprehends professional knowledge with ethical responsibility through current laws and legislation. 1
PLO03 Beceriler - Bilişsel, Uygulamalı Provides consultancy service to patients, community and health care personnel and evaluates advanced knowledge and skills with a critical approach. 1
PLO04 Beceriler - Bilişsel, Uygulamalı Possessing the knowledge of historical and current developments in the field of Pharmacy, monitoring, evaluation and application of scientific and evidence-based data, and adopting lifelong learning. 1
PLO05 Beceriler - Bilişsel, Uygulamalı Have the knowledge and skills to help provide patient-oriented pharmacy applications and individualized pharmaceutical care by learning the basics of Clinical Pharmacy, 1
PLO06 Yetkinlikler - Bağımsız Çalışabilme ve Sorumluluk Alabilme Yetkinliği Takes a role in the evaluation and analysis of the events and cases related to the development of pharmacy profession and education. 2
PLO07 Yetkinlikler - Öğrenme Yetkinliği Integrates and develops professional knowledge via different disciplines and uses the acquired knowledge to improve the health level and quality of life of the community. 2
PLO08 Yetkinlikler - Öğrenme Yetkinliği Use effectively the concepts and applications of basic sciences and basic medical sciences in the field of medicine and pharmacy and update the information. 1
PLO09 Yetkinlikler - İletişim ve Sosyal Yetkinlik Communicates effectively in writing and speaking. 3
PLO10 Yetkinlikler - İletişim ve Sosyal Yetkinlik Practices the profession in accordance with Atatürk's principles and reforms, equipped with universal knowledge, uses Turkish correctly and knows at least one foreign language.
PLO11 Yetkinlikler - İletişim ve Sosyal Yetkinlik Be an example to society withexternal appearance, demeanor, attitude and behavior for the other professionals and society and with professional identity
PLO12 Yetkinlikler - Alana Özgü Yetkinlik Have knowledge about health policies and health economics, pharmacy management and define the problems in pharmaceutical field. 2
PLO13 Yetkinlikler - Alana Özgü Yetkinlik Interprets information about current health and treatment problems and attends meeting on related matters . Plays an active role in community health. 2
PLO14 Yetkinlikler - Alana Özgü Yetkinlik Acquires basic information about diseases, makes decisions about the drugs used in treatment in accordance with rational drug use. 2


Week Plan

Week Topic Preparation Methods
1 Historical backround of drug design and discovery. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
2 Drug-receptor interactions and bond types involved in these interactions. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
3 The role of water/lipid solubility in binding, distribution and metabolism of drugs. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
4 The importance of stereochemistry in drug action, conformationla flexibility, rigid analogs. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
5 The importance of structure-activity relationships for new drug design and the role of acidity-basicity in drug effect. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
6 Approaches used for the definition of lead compound. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
7 Design based on target macromolecules, endogenous molecules, analogue design, combinatorial chemistry. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
8 Mid-Term Exam Repetition of lecture notes Ölçme Yöntemleri:
Yazılı Sınav, Ödev
9 Pharmacophore definition, lead compound modification and optimization Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
10 Bioisosterism, classical and non-classical bioisosters Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
11 Prediction of lipophilicity, ionization and steric parameters. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
12 Pro-drug design, drug targeting and soft drug design. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
13 Drug design based on enzymes, enzyme inhibitors. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
14 Toxic effects due to the functional groups and their correction Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
15 Examples of succesful applications for rational drug design. Reading the relevant lecture note Öğretim Yöntemleri:
Anlatım, Tartışma
16 Term Exams Repetition of lecture notes Ölçme Yöntemleri:
Yazılı Sınav
17 Term Exams Repetition of lecture notes Ölçme Yöntemleri:
Yazılı Sınav


Student Workload - ECTS

Works Number Time (Hour) Workload (Hour)
Course Related Works
Class Time (Exam weeks are excluded) 14 2 28
Out of Class Study (Preliminary Work, Practice) 14 2 28
Assesment Related Works
Homeworks, Projects, Others 0 0 0
Mid-term Exams (Written, Oral, etc.) 1 6 6
Final Exam 1 16 16
Total Workload (Hour) 78
Total Workload / 25 (h) 3,12
ECTS 3 ECTS

Update Time: 06.05.2024 12:33