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Structure-Activity Relationship Expansion

Course Overview

Structure-activity relationship (SAR) studies are a critical part of medicinal chemistry and drug discovery, focusing on understanding how the chemical structure of a molecule correlates with its biological activity. SAR expansion involves systematically modifying the chemical structure of lead compounds to improve potency, selectivity, pharmacokinetics, and safety. Below are key topics and concepts within SAR expansion:

  1. Chemical Substitutions and Functional Group Modification    
  2. Scaffold Hopping
  3. Stereochemistry and Chirality
  4. Ring System Modifications
  5. Topological and Spatial Considerations
  6. Hydrophobic vs. Hydrophilic Balance
  7. Prodrug Design
  8. Fragment-Based SAR
  9. Quantitative SAR (QSAR)
  10. Multi-Target SAR
  11. Lead Optimization
  12. Covalent vs. Non-Covalent Binding
  13. Targeting Allosteric Sites

By applying these principles, SAR expansion allows researchers to systematically refine lead compounds into drug candidates with optimal efficacy, safety, and pharmacological properties.

  • Registration
  • Be contacted to confirm the participation.
  • Scheduling for the program sessions
  • Supplied with the technical support to download the software required for the program.