Provide general principles of medicinal chemistry, evidencing the relationships between drug structure and their therapeutically relevant properties. Analyse the classification, the chemical, physicochemical and biological properties, the mechanism of action, structure-activity relationships and synthesis of main atiinfective and antitumor drugs.
The exams of Organic Chemistry II and General Physiology must be passed before the examination.
Course contents summary
1 - General section 1.1 - Principles of medicinal chemistry Phases of drug action: pharmaceutical, pharmacokinetic and pharmacodynamic phases. Drug disrtibution. Metabolic reactions of drugs. Prodrugs. Drug mechanism of action: theories on drug action; receptors, enzymes and enzyme inhibition; other molecular targets. Chemical and physico-chemical properties vs biological activity. 1.2 - Drug structure and biological activity Specific and non-specific mechanisms of actions. Optical or conformational isomerism and biological activity. Isosterism and bioisosterism; aptophore and pharmacophore fragments. Quantitative structure-activity relationships. 2 - Systematic section Abtibiotics: beta-lactams; macrolides; aminoglycosides; tetracyclines; ansamycins; polipeptides; others.Synthetic antibacterials for systemic use: sulfa drugs, nitro-heterocycles; quinolones, oxazolidinones.Anti-mycobacterials. Antifungals for topic or systemic use: polyenic antibiotics; griseofulvin; thiocarbamates; allylamines; flucytosine; azoles. Antiprotozoals. Antihelmintics. Antivirals.Antitumor drugs: alkylating agents; DNA-binding drugs; antimetabolites; antimitotic agents; topoisomerase inhibitors; TK inhibitors.
Williams-Lemke: "Foye's Principi di Chimica Farmaceutica", PICCIN, Padova.
G.L. PATRICK: Introduzione alla chimica farmaceutica; Edises Napoli.