Course Description
Teaches drug design principles and reactions applied in lead optimization. Topics include non-covalent interactions; lead optimization; chemical space; library design; combinatorial and parallel chemistry; fragment-based drug design; diversity oriented synthesis; asymmetric synthesis; the Suzuki, Buchwald, and related reactions; click chemistry; peptide synthesis; oligonucleotide synthesis; glycodiversification; and green chemistry.
Athena Title
Org Chem Drug Design and Dev
Prerequisite
Permission of department
Semester Course Offered
Offered spring
Grading System
A - F (Traditional)
Course Objectives
Objectives for this course include the instruction of students in the concepts of medicinal chemistry and drug design, including an understanding of the underlying chemical principles and commonly used reaction types so as to prepare them for a career in the biotech and/or pharmaceutical industry, or for entry to a Ph.D. program in the area of synthetic medicinal chemistry
Topical Outline
1. Types of non-covalent interaction between small molecules and their receptors 2. Pharmacophores and isosteres 3. Chemical space and diversity 4. Library design 5. Structure activity relationships 6. Principles of green chemistry as applied to medicinal chemistry 7. Fragment-based drug discovery 8. Lead optimization 9. Combinatorial chemistry and parallel synthesis including polymer-supported synthesis 10. The need for single enantiomers – asymmetric synthesis 11. Main reaction types employed 12. Diversity oriented synthesis 13. Principles of peptide and nucleotide chemistry 14. Glycodiversification
Syllabus