At the end of this course, the students; 1) Stages of drug design and development and reasons for failure in drug development 2) Finding and optimizing the precursor compound 3) Molecular modification, bioisosterism, latent drug design, QSAR and QSAR parameters, combinatorial chemistry and rapid activity screening methods 4) Computer aided drug design 5) Have knowledge of drug repositioning and patents in medicine
MODE OF DELIVERY
Face to face
PRE-REQUISITES OF THE COURSE
No
RECOMMENDED OPTIONAL PROGRAMME COMPONENT
None
COURSE DEFINITION
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
1st 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
2nd Week
Drug design and development stages
/ Finding of a lead compound
3rd Week
Finding of a lead compound: Rational drug design
4th Week
Examples of drugs developed with rational drug design: Cimetidine and captopril
5th Week
Drug design and development stages (continued)
/ Lead optimization: Molecular modifications and bioisosterism
6th Week
Drug design and development stages (continued)
/ Lead optimization: Drug latentiation
7th Week
Drug design and development stages (continued)
/ Lead optimization: Quantitative Structure Activity Relationships (QSAR)
8th Week
Midterm exam
9th Week
Combinatorial chemistry and High-Throughput Screening (HTS)
10th Week
Computer Aided Drug Design (CADD)
11th Week
Cheminformatic, bioinformatic (Protein Data Bank, PDB)
12th Week
Problems and new approaches in drug development
13th Week
Drug repositioning
14th Week
Drug patents
RECOMENDED 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).
