The course is conducted through classroom lectures with slide show and explanations on the blackboard, and aims to provide knowledge about:
• chemical aspects of the action of drugs and prodrugs;
• Chemical considerations in molecular design.
In detail, the course begins with a brief discussion of preliminary issues such as the problem of molecular complexity, the identification of pharmacophores elements and some nods to the synthetic accessibility. It continues with an analysis of the correlations between chemical properties and characteristics biofarmacologiche. Once concluded these preliminary concepts, you proceed to the discussion of "drug-likeness" (or semblance farmacoforica), a subject considered increasingly important in the early stages of drug design, with particular reference to: ADMET parameters, Lipinski / Veber rules and later variants, rule pharmacophoric points. Subsequently, the course focuses on the various aspects of the use of prodrugs. It is treated their structural design, the identification of suitable removable or changeable groups, as well as the main enzymatic and non-enzymatic activations involved. Subsequently they face more complex aspects relating to prodrugs targeted action, such as for example the selective chemotherapeutic to tumor hypoxia to bioriduttiva activation. At the conclusion of the course discusses the main combined strategies that rely on the use of prodrugs and involving selective activation mediated by enzymes (ADEPT, MDEPT, etc.) Or catalytic antibodies (ADAPT). These strategies are then listed the cases that have given the most promising results in clinical trials.