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Information
| Unit | FACULTY OF PHARMACY |
| PHARMACY PR. | |
| Code | ECS518 |
| Name | Drug Active Ingredient Design |
| Term | 2020-2021 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 |
| Label | E Elective |
| Mode of study | Uzaktan Öğretim |
| Catalog Information Coordinator | Dr. Öğr. Üyesi ÖZDEN TARI |
| Course Instructor |
Dr. Öğr. Üyesi ÖZDEN TARI
(Bahar)
(A Group)
(Ins. in Charge)
|
Course Goal / Objective
Presentation of approaches used for 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
Resources
Notes
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 new developments in active substance design. |
| LO03 | The student who completes this course makes literature search on dvelopment of active drug substances. |
| LO04 | The student who completes this course makes 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. | |
| PLO03 | Beceriler - Bilişsel, Uygulamalı | Provides consultancy service to patients, community and health care personnel and evaluates advanced knowledge and skills with a critical approach. | |
| 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. | |
| 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, | |
| 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. | |
| 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. | |
| 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. |
Week Plan
| Week | Topic | Preparation | Methods |
|---|---|---|---|
| 1 | Historical backround of drug design and discovery. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 2 | Drug-receptor interactions and bond types involved in these interactions. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 3 | The role of water/lipid solubility in binding, distribution and metabolism of drugs. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 4 | The importance of stereochemistry in drug action, conformationla flexibility, rigid analogs. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 5 | The importance of structure-activity relationships for new drug design and the role of acidity-basicity in drug effect. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 6 | Approaches used for the definition of lead compound. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 7 | Design based on target macromolecules, endogenous molecules, analogue design, combinatorial chemistry. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 8 | Mid-Term Exam | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 9 | Pharmacophore definition, lead compound modification and optimization | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 10 | Bioisosterism, classical and non-classical bioisosters | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 11 | Prediction of lipophilicity, ionization and steric parameters. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 12 | Pro-drug design, drug targeting and soft drug design. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 13 | Drug design based on enzymes, enzyme inhibitors. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 14 | Toxic effects due to the functional groups and their correction | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 15 | Examples of succesful applications for rational drug design. | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 16 | Term Exams | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. | |
| 17 | Term Exams | Drug discovery handbook, SC Gad (Ed.), John Wiley and Sons, Inc., 2005. Farmasötik Kimya, Hacettepe Üniversitesi Yayınları, 2.Baskı, 2004. Medicinal Chemistry, An Introduction, Gareth Thomas, Wiley. |
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 | ||