Chimie pharmaceutique (Partim) [ WFARM1302P ]

WFARM1231 chimie organique

WFARM1221 biochimie

WFARM1232 pharmacologie générale

WFARM1008 conception du médicament

L'unité d'enseignement suivante devra être acquise ou figurer dans le programme de l'étudiant la même année académique : WFARM1300 (pharmacocinétique et métabolisme des xénobiotiques).

The general theme is the structure - activity relationship of the drugs. Since this theme is broad, it has to be exemplified by selected topics: (i) chemical and physico-chemical properties of drugs in relationship with their pharmacokinetic and pharmacodynamic behavior (phototoxicity, in vitro and in vivo hydrolysis, charge (pKa), logP (Lipinski's rule), chirality) (ii) (ii) ligand - receptor interaction, with regard to physico-chemical properties : ature of the intermolecular interactions, types of targets (receptors, ion channels, enzymes, transporters, pumps), consequence of the binding of a xenobiotic on these targets (iii) drug discovery and optimization process, scope and limitation of the drug design techniques. The practical exercises allow students to establish themselves their own experimental plans in order to assign the structure of simple molecules (spot tests, derivatization, spectroscopy).

At the end of this formation, students are able to make a link between a drug structure and the interaction of this drug with the living, and establish structure - pharmacological activity relationships (drug design, potential actions of a molecule on a given receptor) as well as structure - pharmacokinetic behavior relationships (crossing of physiological barriers, pKa, logP, chemical and photochemical stability). The practical exercises aim at assuring the transition between those of FARM1230 and FARM2205: students must be able to design a rational experimental plan