Ateneo - UPO

The course deals with the in-depth study of different classes of drugs, considering the rationale behind their discovery, the mechanism of action, the structure-activity relationships, and the therapeutic use. In particular we will consider the following classes of drugs:
Cardiovascular agents;
Drug actin on the renal system;
Prostaglandins, leukotrienes, and essential fatty acids;
Histamine and antihistaminic agent;
Antiulcer agents;
Steroid hormones and therapeutically related compounds.
anti-cancer, anti-bacterial, anti-viral.

A. Gasco, F. Gualtieri, C. Melchiorre Chimica Farmaceutica (I Eds.) Casa Editrice Ambrosiana;
W. Foye, Principi di Chimica Farmaceutica, Piccin; (VI Eds.);
Wilson and Gisvold, Chimica Farmaceutica (I Eds.) Casa Editrice Ambrosiana;
G.L. Patrick Introduzione alla Chimica Farmaceutica (edizione integrata) EdiSES.
T.L. Lemke, D.A. Williams. Foye’s, Principi di Chimica Farmaceutica, V Eds. Piccin.

The goals of the course of Medicinal Chemistry and Drug Design II are:
- To provide students with the fundamental knowledge of the drug classes discussed and at the same time the general strategies for their design, the study of their mechanisms of action at the molecular level, their chemical- toxicological aspects and their relationships between chemical structure and biological activity. At the end of the course, the student will have gain a deep knowledge concerning these classes of drugs, in particular with regard to their mechanism of action at the chemical level. At the end of the course, the student will be able to read, in a critical manner, books and scientific articles regarding these classes of drugs.

Regarding preparatory Pharmaceutical Chemistry and Drug design I
Preliminary matters Knowledge in the field of Organic Chemistry, General Pathology, Biochemistry, Physiology, Pharmacology.

Frontal Seminar

The learning assessment consists of a written examination. The questions cover all the topics which have been discussed during the lessons.

Cardiovascular agents. positive inotropic, antianginal, antiarrhythmic agents, diuretics, ACE inhibitors, calcium channel modulators, central and peripheral sympatholytic agents, vasodilators, inhibitors of cholesterol biosynthesis and antilipoproteinemici; design and synthesis of agents of the cardiovascular system, the search for new agents for the cardiovascular system
Agents that interfere with the hormone system (corticosteroids, glucocorticoids, male and female sex hormones). Nomenclature, structure, mechanisms of action, biosynthesis and metabolism. Drugs that act on receptors SAR steroids. Antagonists of steroids, mechanism of action, design and synthesis. Nonsteroidal anti-inflammatory drugs, antihistamines and anti-allergy drugs. Design and synthesis of NSAIDs and H1 antihistamines, the search for new NSAIDs and antihistamines H1. Histamine receptor H1, H2, H3 and H4 ligands.
Antisecretory agents: H2 antihistamines, proton pump inhibitors. Design and synthesis of H2 antagonists and proton pump inhibitors.

Module B
Antibacterial agents. The giants of the past: Leeuwenhoek, Spallanzani, Pasteur, Lister, Kock. The bacterial cell. Gram + and Gram -. The bacterial cell wall. Proflavine. Sulfonamides. The problem of the resistance. Sulphones. Diidrofolate reductase inhibitors. Penicillins. Cephalosporins. Carbapenenms. Monobactams. Beta-lactamase inhibitors. Other antibiotics which act on bacterial cell wall. Antibacterial agents which act on the plasma membrane. Antibacterial agents which impair protein synthesis. Antibacterial agents which act on nucleic acids. Antitubercular drugs. Antiprotozoal drugs. Antimalarian drugs. Antifungal drugs. Anthelmintic drugs.
Anticancer drugs. Cancer: an introduction. Causes of cancer. Antimetabolites. Drugs acting on nucleic acids. Drugs acting on tubulin. Hormone-based terapies. Kinases inhibitors.Miscellaneous enzyme inhibitors.
Antiviral agents. Virus. Structure of virus. Life cycle of virus. Antiviral drugs against DNA virus. Antiviral drugs against RNA virus. Hiv virus and drugs.Antiviral drugs against flu virus. Antiviral drug against cold virus. Antiviral drugs against hepatite virus.

The students at the end of the course will know fundamental aspects regarding specific drug classes. In particular, the student will be able to recognize the general strategies for their design, the study of their mechanisms of action at the molecular level, their chemical- toxicological aspects and their relationships between chemical structure and biological activity. As ultimate goal the student will be able to read, in a critical manner, scientific articles regarding these classes of drugs.