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| ECZ2039 | Basic Principles of Medicinal Chemistry | 2+0+0 | ECTS:4 | | Year / Semester | Fall Semester | | Level of Course | Second Cycle | | Status | Elective | | Department | DEPARTMENT of PHARMACEUTICS | | Prerequisites and co-requisites | None | | Mode of Delivery | | | Contact Hours | 14 weeks - 2 hours of lectures per week | | Lecturer | Dr. Öğr. Üyesi Hasan Erdinç SELLİTEPE | | Co-Lecturer | | | Language of instruction | Turkish | | Professional practise ( internship ) | None | | | | The aim of the course: | | The main objective of this course is to teach students the basic principles of medicinal chemistry, such as functional groups and their properties, the acid-base character of the drug molecule, pH and pKa concepts, and the first steps of rational drug design. It also aims to teach the basic dynamics of the relationship between basic modifications on the molecule and pharmacological activity. |
| Learning Outcomes | CTPO | TOA | | Upon successful completion of the course, the students will be able to : | | | | LO - 1 : | Defines the functional groups on the molecule and has information about their physicochemical properties. | 1,2,4 | 1, | | LO - 2 : | Learns the parameters that have an important affect in the biological activity of drugs such as stereochemistry and bond types. | 1,2,4 | 1, | | LO - 3 : | Have basic information about structure-activity relationship. | 1,2,4 | 1, | | CTPO : Contribution to programme outcomes, TOA :Type of assessment (1: written exam, 2: Oral exam, 3: Homework assignment, 4: Laboratory exercise/exam, 5: Seminar / presentation, 6: Term paper), LO : Learning Outcome | | |
| Basic concepts in medicinal chemistry; functional groups and their properties, acidic and basic groups, pH and pKa, salts and solubility, drug binding interactions, stereochemistry and drug activity, drug metabolism, structure-activity relationship.
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| Course Syllabus | | Week | Subject | Related Notes / Files | | Week 1 | What is medicinal chemistry?
Basic concepts.
| | | Week 2 | Functional groups and their properties: steric, electronic and solubility properties.
Problems | | | Week 3 | Functional groups and their properties: steric, electronic and solubility properties.
Problems | | | Week 4 | Acidic functional groups.
Basic functional groups.
| | | Week 5 | Relationship between acidic-basic character and therapeutic effect.
Problems | | | Week 6 | The concept of pH and pKa.
Henderson-Hasselbach equation. | | | Week 7 | Problems encountered with pH and pKa in drug molecules.
Problems | | | Week 8 | Organic and inorganic salts. | | | Week 9 | Midterm | | | Week 10 | Salts and solubility.
Partition coefficient. | | | Week 11 | Advantages and disadvantages of water/lipid solubility
Effect of solubility on drug metabolism. | | | Week 12 | Covalent and noncovalent bonds. | | | Week 13 | Covalent and noncovalent bonds. | | | Week 14 | Drug binding interactions.
| | | Week 15 | Structure-activity relationship. | | | Week 16 | Final exam | | | |
| 1 | Foye Medisinal Kimya Temel İlkeleri. 2019. David A. Williams , S. William Zito , Thomas L. Lemke , Victoria F. Roche. Çeviri Editörü: Dr. Ecz. Kayhan BOLELLİ , Prof. Dr. Öztekin ALGÜL | | | 2 | Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry - John M Beale, John Block. | | | 3 | Basic Concepts in Medicinal Chemistry - Marc W. Harrold , Robin Zavod. | | | 4 | An Introduction to Medicinal Chemistry - Graham L. Patrick | | | |
| Method of Assessment | | Type of assessment | Week No | Date | Duration (hours) | Weight (%) | | Mid-term exam | 9 | 26.11.2023 | 1 | 50 | | End-of-term exam | 16 | 25.01.2024 | 1 | 50 | | |
| Student Work Load and its Distribution | | Type of work | Duration (hours pw) | No of weeks / Number of activity | Hours in total per term | | Yüz yüze eğitim | 2 | 14 | 28 | | Arasınav için hazırlık | 5 | 7 | 35 | | Arasınav | 1 | 1 | 1 | | Dönem sonu sınavı için hazırlık | 6 | 7 | 42 | | Dönem sonu sınavı | 1 | 1 | 1 | | Total work load | | | 107 |
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