Medicinal Chemistry is an interdisciplinary science, students should gather good skills in organic chemistry (OC) and a background in biochemistry and biology. The aim of the CU is to integrate chemical biology and OC to reveal how they are used in MedChem, design and synthesize new drugs and understand their mode of action MoA.
Objectives on teaching /learning are to promote the acquisition of scientific knowledge and develop thinking skills /criticism so that it can:
-Establish strategies/employ the most current methodologies in the discovery, design and pharmacodynamic /kinetic optimization of new drugs;
-Understand molecular parameters/chemical mechanisms involved in the absorption/metabolism of drugs and assess the impact on bioavailability;
- Interpret structure-activity relationships and apply the findings in prototype optimization;
-Understand the chemical MoA of drugs.
- Apply the chem. /molecular bases of drugs action to the rational design of novel therapeutic agents.
The central core of the discipline is the description of methods used for the discovery of new drugs, how these are modified to produce more active compounds. Topics covered include:
Molecular properties and Pharmacokinetics: pH and drug absorption. Drug metabolism. Toxicity and drug interactions.
Important fragments of drugs and drug targets: Nucleic acids. Carbohydrates. Lipids. Amino-acids, peptides and proteins.
Drug discovery and design: Strategies in lead discovery. Optimizing target interactions; chemical modification and structure-activity relationships (SAR) and QSAR. Combinatorial and parallel synthesis. Computer-assisted drug discovery and design. Prodrugs and others chemical modifications.
Enzymes as therapeutic targets:Kinetics and mechanism of action of reversible and irreversible enzyme inhibitors. Enzyme inhibitors as pharmacodynamic therapeutic agents.Examples.
Nucleic acids as therapeutic targets. DNA-interactive agents