00126 - Medicinal and Toxicological Chemistry I;

Course contents

GENERAL PART
Definition of medicinal chemistry. Process of action of drugs. Molecular targets of drugs. Interaction between a drug and a molecular target: bonds involved in the interaction. Stereochemistry and drug action: optical, geometrical and conformational isomerism. Pharmacokinetic phase: absorption, distribution, elimination; metabolism: phase I and phase II reactions. Introduction to drug design.

DESCRIPTIVE PART
Drugs acting on the biosynthesis of the cell wall: beta-lactam antibiotics; peptide antibiotics; isoniazide, ethambutol.
Drugs acting on the function and biosynthesis of components of the cell membrane: peptide antibiotics; macrolide-polyene antibiotics; azoles, allylamines.
Drugs acting on the protein biosynthesis: tetracyclines; aminoglycosides; macrolide antibiotics; ansamycins.
Drugs acting on the DNA biosynthesis: sulfonamides; diamino-pyrimidines, -triazines and analogues; purines, pyrimidines and analogues.
Drugs acting on DNA: nitrogen mustards, nitrosoureas, ethyleneimines, mitomycins, platinum derivatives; pentamidine, distamycin and analogues; actinomycins, quinolines, acridines; anthracyclines and derivatives; quinolones.
Drugs acting on mitosis: Vinca alkaloids; taxol derivatives.
Drugs acting on the eicosanoids system: nimesulide, coxibs; salycilic and anthranylic acid derivatives; acetic and propionic acid derivatives; pyrazolidindiones; benzothiazines; pyrazolinones; acetanilides.
Drugs acting on the steroid hormones system: estrogens; androgens; progestins; glucocorticoids; mineralocorticoids.

Readings/Bibliography

G.L. PATRICK Introduzione alla Chimica Farmaceutica. Seconda Edizione
EdiSES, Napoli, 2010 (ed. originale 2009)

G. GRECO Farmacocinetica e Farmacodinamica su Basi Chimico-Fisiche
Loghìa, Napoli, 2007

D.A. WILLIAMS, T.L. LEMKE (Eds.) Foye's Principles of Medicinal Chemistry. Fifth Edition
Lippincott Williams & Wilkins, Philadelphia, 2002
(Ed. italiana, Piccin, Padova, 2005)

M.E. WOLFF (Ed.) Burger's Medicinal Chemistry and Drug Discovery. Fifth Edition
John Wiley & Sons, New York, 1995

C. HANSCH (Ed.) Comprehensive Medicinal Chemistry
Pergamon Press, Oxford, 1990

D. LEDNICER, L.A. MITSCHER The Organic Chemistry of Drug Synthesis, voll. 1-6
John Wiley & Sons, New York, 1977, 1980, 1984, 1990, 1995, 1999

R.B. SILVERMAN The Organic Chemistry of Drug Design and Drug Action
Academic Press, San Diego, 1992

F. GUALTIERI (Ed.) New Trends in Synthetic Medicinal Chemistry
Wiley-VCH, Weinheim, 2000

C.G. WERMUTH (Ed.) Le applicazioni della Chimica Farmaceutica
EdiSES, Napoli, 2000 (ed. originale 1996)

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