Course name: Principles of medicinal and toxicological chemistry
COURSE CONTENT
Structure-activity relationships, mechanism and site of action, therapeutic use, side effects, stereochemistry, of selected drugs.
Receptors: structure and function. Classification of receptors. General mode of operation. Ligand-response relationships: agonist, antagonist, partial agonist, and inverse agonist. Enzymes as target for selected drugs.
Drug affecting cholinergic neurotransmission: muscarinic and nicotinic; agonists and antagonists. Acetylcolinasterase inhibitors. Drug affecting adrenergic neurotransmission: α and β receptors. Drug affecting serotoninergic neuro transmission. Sedative hypnotic. Anxiolytic agents. Antiseisure agents. Antidepressants. Drugs for neuromuscular disorders. Antiparkinson Agents. Hallucinogens, stimulants and related drugs of abuse. Antpsychotic agents. Antihistamines and related antiallergic and antiulcer agents. Local anesthetics. General anesthetics. Opioid analgesic. Drugs for Alzheimer disease. Analeptic pneumocynetic. Adrenocorticoids. Gluco and mineral corticoides. Estrogens, progestins and androgens. Steroid hormone antagonists. Oral contraceptives. Antihyerlipoproteinemics and inhibitors of cholesterol biosynthesis.
Chemiotherapeutics agents.
Antibiotics interfering with the biosynthesis of the bacterial cellular wall: beta-lactams antibiotics Penicillins. Cephalosporins: Thyenamycins, Imipenem., clavulanic acid.
Antibiotics interfering with the protein transcription: Ansamycins (Rifamycins).
Antibiotics interfering with the (protein transduction: Macrolides, Chloramphenicol ,aminoglycosides, Tetracyclines .
DNA gyrase inhibitors: Quinolones. Antimalaric drugs:Plasmodium life cycle. Antimycotics drugs: natural antimycotics: Griseofulvin, Macrolides Polyenes .Synthesic Antymicotics: Azoles (mode of action), Allylammines, thiocarbammates, 5-Fluorocitosine.
Antiviral drugs: Derivatives of purines and pyrimidines. Ribavirin. Foscarnet. Protease inhibitors.Inhibitors of integrase.
Anticancer drugs: Alkylating drugs. Antimetabolites. Intercalators. Topoisomerase I and II inhibitors. Mitotic inhibitors.
Steroidal hormones: estrogens, androgens, mineralcorticoids and glucocorticoids.Antagonists of Steroidal hormones.
Arachidonic acid cascade: prostaglandins, thromboxanes and leukotrienes.
Non steroidal antinflammatory drugs: mode of action, SAR, pharmacological profile, (COX 1 and COX 2 selectivity). Salicylic acid derivatives. Arylacetics and arylpropionics, oxycams.
LEARNING OUTCOME
Knwledge and ability to acquire
The objectives of the teaching course are to supply to the student the fundamental knowledge of the mechanism of action at molecular level and the relationships between the molecular structure and the biological activity and the side effects of synthetic, natural and biotechnological drugs, able, in general, to interact with receptors and enzymes..
It is reasonable to take into account that the student acquires the ability to discuss the mechanisms of action, the relationships structure-activity and the side effects of the drugs. Moreover he should know the problems concening the clinical trials and the immission in the marked of the new drugs.
CREDITS: 8
CONTACT INFORMATION
Prof. Francesco Dall'Acqua:
049 8275708, e-mail:
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Department of Pharmaceutical Sciences, Ed. B. First Floor, Via Marzolo 5, 35131, Padova
Office Hours: Tuesday and Wednesday 10-11 a.m., otherwise upon appointment via e-mail or phone