Drug Design and Synthesis

Recommended Prerequisites

Frequency and approval in the discipline of Biomolecular Organic Chemistry and Therapeutical Chemistry Knowledge of Organic Chemistry
Knowledge of English.

Teaching Methods

The theoretical classes will be taught by the projection of slides, which are then placed on the platform nónio.
The theoretical-practical classes will be taught by projection of slides and with the active participation of students in problem solving and in work presentation, individually or in groups.

Learning Outcomes

-Locate the chronologically development of drugs
-Defining the concept of drug and studying the various types of targets
-Analyze the different bonds involved in the interaction of the drugs with their targets
-Identify the pharmacophore and set the auxophore and toxophore
-Set the basic principles associated with the synthesis of drugs
-Studying the main control techniques of preparation reactions and structural elucidation of drugs
-To know the main strategies of drug design
-To interpret the principles of analog design
-To know predict the chemical modifications more likely for the interactions with molecular targets
-To know the basics of different spectroscopic methods and utilize the information obtained in structural elucidation of organic compounds
-Apply properly the principles and key points governing the disconnection approach.
-Be able to, based on the performed disconnection, design the reverse synthesis applying the appropriate transformation of functional groups.

Work Placement(s)

No

Syllabus

THEORETICAL TEACHING:
- Reference to the history of Drug Discovery
- The drug and its interaction with molecular targets
- Molecular drug targets
- Complementarity between molecular target and drug
- Basic principles associated with the synthesis of drugs- Chromatographic and spectroscopic techniques to control reactions and to elucidate the structure of the products formed
- Rational drug design strategies
- Drug design based on pharmacofore and on receptor
- Analog design principles
- Isosterism and bioisosterism concepts, “Scaffold Hoping” and vinylogy
- Drug Synthesis: Different issues involved in drug synthesis.
- The Retrosynthetic approach as a strategy planning to achieve the target molecule.
- Synthesis and interconversions of organic compounds.
- “Case Studies”
THEORETICAL-PRACTICAL TEACHING:
Solving exercises on the subjects studied in the theoretical teaching.

Head Lecturer(s)

Saúl Campos Pereira Costa

Assessment Methods

Assessment
Research work: 20.0%
Exam: 80.0%

Bibliography

• Erland Stevens, MEDICINAL CHEMISTRY - The Modern Drug Discovery Process. Copyright © 2014
by Pearson Education, Inc.
• Graham L. Patrick, An Introduction to DRUG SYNTHESIS, Jan 2015. OXFORD University Press.
• The Practice of Medicinal Chemistry (3ª Ed.) Edited by Camille-Georges Wermuth.
• Andrew Rosen, Organic Chemistry: Reactions and Overview. Editor: Raghav Malik, 2013.
• THE ART OF DRUG SYNTHESIS, Edited by Douglas S. Johnson and Jie Jack Li. Pfizer Global Research
and Development. Copyright © 2007 by John Wiley & Sons, Inc.
• ORGANIC CHEMISTRY, Francis A. Carey, Robert M. Giuliano, McGraw-Hill; 8th edition (2010).