MEDICINAL CHEMISTRY I
cod. 07559

Academic year 2009/10
2° year of course - Second semester
Professor
Academic discipline
Chimica farmaceutica (CHIM/08)
Field
Discipline chimiche
Type of training activity
Characterising
64 hours
of face-to-face activities
8 credits
hub:
course unit
in - - -

Learning objectives

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.

Prerequisites

Biochemistry, General Physiology

Course unit content

<br />GENERAL PART<br />Introduction Illustration of the aims of the course. Definition, classification and nomenclature of drugs. Strategies for drug discovery. Optimization of the lead compound.<br />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.<br />Drug metabolism  Drug biotransformation; phase I and phase II reactions; the cytochrome P-450 system. Prodrugs.<br />SYSTEMATIC PART<br />Drugs primarily acting upon the Peripheral Nervous System<br />Cholinergics Parasympathomimetics and parasympatholytics. Anticholinesterase drugs. Nicotinic antagonists: ganglionic blocking  agents and neuromuscular blocking agents.<br />Adrenergics Sympathomimetics and sympatholytics.<br />Cardiovascular drugs<br />Cardiotonics, antianginal drugs, antiarrhythmic drugs, antihypertensives. Lipid-lowering  drugs.<br />Anti-infectious drugs<br />Current state of control of infectious diseases. Chemiotherapics and antibiotics.<br />Synthetic systemic anti-infectious drugs. Sulfamidics, nitro heterocycles, quinolones.<br />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.<br />Antiviral drugs<br />General. Cyclic amines, thiosemicarbazones, biguanides, purine and pyrimidine antimetabolites, interferon.<br />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.<br />Anti-cancer drugs<br />General. Principles of cancer chemotherapy.<br />Cancer chemotherapics. Alkylating, intercalating and DNA complexing agents. Antimetabolites. Antimitotic drugs. New approaches in cancer treatment. Notes on immunotherapy and on bio-drugs.<br /><br />

Full programme

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Bibliography

<br /><br /><br />D.A. Williams, T.L. Lemke  Foye's Principi di Chimica Farmaceutica  Ed. Piccin Bologna<br />  E. Schroder, C.Rufer, R.Schmiechen Chimica Farmaceutica EdiSES - Napoli <br /> C.G. Wermuth Le applicazioni della Chimica Farmaceutica  EdiSES - Napoli<br />  G.L. Patrick Introduzione alla Chimica Farmaceutica EdiSES - Napoli<br />

Teaching methods

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.

Assessment methods and criteria

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Other information

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