Chemistry

General Module Receptor theories and chemical-physical bases (bonds) of drug-receptor interactions. Pharmacokinetic and pharmacodynamic parameters for rationalizing therapeutic activity. Classification of the main classes of receptor systems (cholinergic, adrenergic, GABA-ergic, dopaminergic, serotonergic, histaminergic, opioid, phosphodiesterase) with elements of therapeutic activity. Concepts of agonist, partial agonist, and antagonist. Drug Synthesis Module Main classes of reactions commonly used in pharmaceutical synthesis. Stereochemical aspects and chirality induction Carbon nucleophilic reagents (Grignard, organolithium, organozinc, organocopper, organomanganese, organosilicon): preparation, reaction mechanisms, and use in pharmaceutical synthesis. Reactions catalyzed by transition metals (palladium, copper, nickel) and their applications in pharmaceutical synthesis. General reaction mechanisms and aspects of reactivity implementation for pharmaceutical synthesis. Homologation reactions. Chemistry of sulfur ylides and diazomethane with applications to drug synthesis. Carbenoids and modulation of nucleophilic or electrophilic reactivity: use in carbon chain elongation and cyclopropanation reactions. Nucleophilic or electrophilic introduction of the fluorine atom into organic molecules. Total synthesis of biologically active products of natural origin.

In-depth knowledge of basic organic chemistry.

Didactic materials provided by the Lecturer. Notes from lectures.

Optional attendance but strongly suggested.

Oral examination with the Lecturer.

R. B. Silverman The Organic Chemistry of Drug Design and Drug Action, Elsevier, 2004, Burlinton. D. S. Johnson, J. J.-Li The Art of Drug Synthesis, John Wiley and Sons, 2007, Hoboken.

Frontal lectures facilitated by blackboard and eventual slides.