|
Lecturer(s)
|
|
|
|
Course content
|
The subject "Basic principles of drug design" is focused on theoretical and practical aspects of the discovery process of novel biologically active compounds and their development to clinical trials. The main goal of the subject is to explain the general routines used in the search for novel structural types of biologically active compounds and their modification to candidates suitable for further clinical development (hit-to-lead process). The students will be acquainted with common techniques including the classical approaches such as extensive, random and high-throughput screening as well as modern methodologies of the rational drug design based on our knowledge of molecular targets of important human pathogens and the use of computational methodologies for their exploration. Several important topics related to structure-activity relationship will be discussed in detail. Firstly, the discussion should focus on the importance of homology and alteration of the size and shape of hydrocarbon chains for the design of new structural analogues. Secondly, the terms isosterism and bioisosterism will be explained and their crucial role in optimization of pharmacodynamic parameters will be demonstrated. The subject should also explain the influence of stereochemistry and conformational properties on the biological activity of new drugs. Special attention will be given to the importance of pharmacokinetic parameters and their alteration by chemical methods. Students should be familiarized with techniques leading to the increase in solubility and bioavailability of novel remedies. Finally, practical methodologies of modern combinatorial medicinal chemistry will be demonstrated on high-speed solution and solid-phase synthesis, preparation of libraries of organic compounds with potential biological activities and high-throughput purification methodologies. The presented information should be supported by numerous examples of design and development of interesting or clinically successful compounds such as novel antiviral and cytostatic agents, modern psycho pharmaceuticals and antihypertensive drugs.
|
|
Learning activities and teaching methods
|
|
Lecture
|
|
Learning outcomes
|
The primary objective of the subject Basic principles of drug design is to familiarize students with practical methodologies used for design and development of new drugs as well as with diverse strategies leading to enhancement or modification of their biological activities.
Students of the subject should embrace the basic principles and skills of the modern design of biologically active compounds and optimization of their structure.
|
|
Prerequisites
|
unspecified
|
|
Assessment methods and criteria
|
Written exam
The subject is intended for advanced students of master's degree interested in practical aspects of design and development of new drugs, namely to students of Chemistry, Bioorganic chemistry and Biochemistry.
|
|
Recommended literature
|
-
Abraham, D. J. Burger's. Medicinal Chemistry, Drug Discovery and Development (Sixth edition or Seventh edition) Wiley, New York, 2010..
-
Wermuth, C. G. (2015). The Practice of Medicinal Chemistry, 4th ed.. Elsevier Science.
|