MEDICINAL CHEMISTRY I
Learning outcomes of the course unit
Knowledge of the basic principles of pharmaceutical research. Illustration of selected classes of drugs: drugs that act on the peripheral nervous system; cardiovascular drugs; anti-infectious drugs; anticancer drugs.
Biochemistry, General Physiology
Course contents summary
Introduction Illustration of the aims of the course. Definition, classification and nomenclature of drugs. Strategies for drug discovery. Optimization of the lead compound.
Pharmacological structure and activity Phases of a drug's action. Mechanism of the molecular action of drugs. Chemico-physical properties and biological activity. Receptors and drug-receptor interactions. The binding interactions of the drug-receptor complex. Receptor theories. Enzymes and enzyme inhibitors. Antimetabolites. Stereochemistry and pharmacological activity. Optical, geometric and conformational isomerism. Isosterism and bioisosterism.
Drug metabolism Drug biotransformation; phase I and phase II reactions; the cytochrome P-450 system. Prodrugs.
Drugs primarily acting upon the Peripheral Nervous System
Cholinergics Parasympathomimetics and parasympatholytics. Anticholinesterase drugs. Nicotinic antagonists: ganglionic blocking agents and neuromuscular blocking agents.
Adrenergics Sympathomimetics and sympatholytics.
Cardiotonics, antianginal drugs, antiarrhythmic drugs, antihypertensives. Lipid-lowering drugs.
Current state of control of infectious diseases. Chemiotherapics and antibiotics.
Synthetic systemic anti-infectious drugs. Sulfamidics, nitro heterocycles, quinolones.
Antibiotics. General. Beta-lactams (penicillin, cefalosporins, fused-ring and isolated-ring analogs, macrolides (antibacterial macrolides, polyenes, ansamycins), polypeptides, aminoglucosides, tetracyclines, chloramphenicol, miscellaneous antibiotics. Antineoplastic antibiotics.
General. Cyclic amines, thiosemicarbazones, biguanides, purine and pyrimidine antimetabolites, interferon.
Anti-AIDS drugs. General. Classes of substances with anti-HIV activity: Enzymes inhibitors, binding inhibitors and inhibitors of viral uncoating; inhibitors of gene expression (anti-sense oligonucleotides). New developments in anti-HIV treatment.
General. Principles of cancer chemotherapy.
Cancer chemotherapics. Alkylating, intercalating and DNA complexing agents. Antimetabolites. Antimitotic drugs. New approaches in cancer treatment. Notes on immunotherapy and on bio-drugs.
D.A. Williams, T.L. Lemke Foye's Principi di Chimica Farmaceutica Ed. Piccin Bologna
E. Schroder, C.Rufer, R.Schmiechen Chimica Farmaceutica EdiSES - Napoli
C.G. Wermuth Le applicazioni della Chimica Farmaceutica EdiSES - Napoli
G.L. Patrick Introduzione alla Chimica Farmaceutica EdiSES - Napoli
The final exam focuses on all the topics included in the course syllabus. The student must demonstrate that he/she has understood the fundamental concepts of each topic and that he/she is able to use them.