| Topic |
Sub-topic |
| Chapter 1. General aspects. Nomenclature and clasification of drugs. |
Main concepts. Key steps in drug development. Drug lassification. Drug nomenclature. |
| Chapter 2. Interactions between the drugs and their biological targets. |
Introduction and main concepts. Biological targets: lipids, carbohydrates, proteins (enzimes and membrane receptors) and nucleic acids. Interactions between drug and the biological target. Molecular topology and biological activity. |
| Chapter 3. Pharmacokinetics. Physicochemical properties of the drugs. |
Introduction. ADME processes. Nature of the biological membranes. Transport across the biological membranes. Farmacokinetic factors. |
| Chapter 4. Metabolic processes of the drugs. |
Introduction. Characteristics of the drug metabolism. Phase I metabolic processes: Oxidation, reduction and hydrolisis reactions. Phase II metabolic processes: Conjugation with glucuronides, sulphate, aminoacids and glutation reactions, acetylation and methylation reactions. Consecuences of the metabolic processes. Stereoselectivity of the metabolic processes. |
| Chapter 5. Steps in the search and discovery of new drugs. |
Main steps in the search of new drugs. Choice of the illness, the biological target and the bioassay. Search of the hit: from natural sources, systematic screening, improvement of previous drugs, rational design, casual discovery of drugs, etc. SAR relationships and identification of the pharmacophore. |
| Chapter 6. Main strategies of pharmacomodulation. |
Objectives of the pharmacomodulation. Strategies of the pharmacomodulation. Pharmacokinetics and pharmacodynamic modulation. |
| Chapter 7. Prodrugs and their applications. |
Definition. Classification of the prodrugs. Examples of each kind and application. Controlled desactivation drugs. |
| Chapter 8. Introduction to heterocyclic systems with therapeutic interests. |
Importance of the heterocycles. Nomenclature. |
| Chapter 9. Structure and reactivity of the main heterocyclic systems. |
Aromatic heterocycles: Pi-excedent heterocycles and pi-deficient heterocycles. Pyrroles, thiophenes and furans. Azoles. Condensed five membered heterocyclic compounds: indole. Six membered heterocycles containing an oxygen atom. Pyridines, Chinolines and isochinolines. Diazines. |
| Chapter 10. General rules in the synthesis of heterocycles. |
General concepts in organic synthesis. General rules in the synthesis of heterocyclic systems. |
| Chapter11. Most used strategies in the synthesis of heterocycles. |
Ring forming ionic cyclization. Synthesis using pericyclic reactions. Chemical modification of the ring. |
Subjects