CHEM 4670 - Drug Design and Drug Discovery

The course will give the student an understanding of the design, synthesis and interactions of drug molecules. Emphasis will be on the organic chemical principles and reactions vital to drug design and drug action. Upon completion of the course, the student should be able to demonstrate an understanding of the concepts involved in drug design and drug interactions, drug synthesis and biological evaluation.

Topics to be covered

Drug Discovery, Design and Development
Drug Discovery, Lead Modification, Drug Design and Development Quantitative Structure-Activity Relationships

Introduction, Drug-Receptor Interactions, Interactions involved in the Drug Receptor Complex, Determination of Drug Receptor Interactions, Theories for Drug-Receptor Interactions, Topographical and Stereochemical Considerations

Enzymes as catalysts, Mechanisms of Enzyme catalysis, Coenzyme Catalysis

Enzyme Inhibition and Inactivation
Introduction, Drug Resistance, Drug Synergism, Reversible Enzyme Inhibition, Irreversible Enzyme Inhibition

DNA-Interactive Agents
Introduction, DNA Structure and Properties, Classes of Drugs that interact with DNA

6. Drug Metabolism/Drug Delivery

CHEM 3580 - Methods in Physical Organic Chemistry

This course deals with the application of physical principles to organic chemistry. We will have a detailed look at reaction mechanisms, intermediates and transition states. This course requires successful completion of a lab section.

Topics to be covered

Methods of Studying Organic Reactions
Identification of reaction products, intermediates, trapping of intermediates, crossover experiments, isotopic labeling, solvent effects, solvent polarity, Kossower scale, review of kinetics, energetics, Arrhenius theory, Eyring transition state theory, kinetic/thermodynamic control, kinetic isotope effect, Hammett plots, free energy relationships

Chemistry of Reactive Intermediates
Structure, stability of carbocations, carbanions, radicals, carbene/carbenoids, generation of intermediates, reaction of intermediates, rearrangement reactions of intermediates, anchimeric assistance, non-classical carbocations, intimate ion pairs, internal return, salt effects

Acid-Base Catalyzed Reactions
Acidity in solution and in the gas phase, pKa and pKb values, general acid/base catalysis, enzymatic hydrolysis of glycosides, Aldol reactions, ester hydrolysis (AAc2, AAc1, AAl1, BAc2, AAc1, AAl1 reactions), acetal hydrolysis, stereoelectronic effects, amide hydrolysis, nucleophilic catalysis, enzyme models

Pericyclic Reactions
Electrocyclic reactions (Woodward-Hoffmann rules, Frontier-Orbital Theory, correlation diagrams), thermal cycloaddition reactions (correlation diagrams, secondary orbital effects, photochemical cycloaddition reactions)

Special Topics
To be decided

LAST UPDATE: September 2013

Dr. Frank Schweizer
Associate Professor
Departments of Chemistry
and Medical Microbiology
University of Manitoba
Winnipeg, MB
R3T 2N2

Office:460 Parker
Labs: 448 & 446 Parker

Tel: (204) 474-7012
Fax: (204) 474-7608

CHEM 7450 - Recent Developments in Organic and Carbohydrate Chemistry