Catalogo dei Corsi di studio

Aim of the subject is to provide the student with the rational basis of Medicinal chemistry and give him the specific chemical knowledge of the drug therapeutic activity. The subject consists in two sections including general medicinal chemistry and systematic medicinal chemistry. The general section analyses the concepts, the strategy of the drug design and discovery for marketplace and the rules of systematic naming of drugs. Knowledge of pharmaceutic and pharmacokinetic phases allows to understand the drug route inside the human body from absorption to distribution. The pharmacodynamics phase analyses the different drug targets, and tries to explain the binding interactions of the drug with the molecular target. The medicinal chemistry systematic section consists in the description of natural and synthetic antimicrobial agents, including sulphamidics, quinolones, nitrochemotherapeutic agents, antibiotics inhibitors of peptidoglycan synthesis, penicillins, cephalosporins, carbapenams, antibiotics inhibitors of ribosome, aminoglycosides, macrolides, tetracycline, chloramphenicol, ansamicyns; antifungal agents, antimycobacterial agents, antivirals, anticancer drugs, antinfective agents, and drugs of the gastrointestinal tract. Inside each drug class, the study of the drug discovery and development processes, the mechanism of action at molecular level, the structure-activity relationships, the metabolism and the synthesis of selected drugs play key roles. The learning route leads the student to manage the chemical knowledge of the drug action. The student can understand the drug distribution inside the human body, the drug interaction with the target and the drug metabolism. The subject provides the student with basis at chemical level of the drug action of each drug class, the chemical manipulation to expand the spectrum of activity, to improve efficacy and tolerability.

Programme

The subject “Chimica farmaceutica e tossicologica I” leads the student to acquire the basis of knowledge to understand the therapeutic action of the drug at a chemical level. At the end of this subject, the student can understand the sequence of events inside the human body from drug administration to excretion. As a guide to learning fruitful, this subject was splitted into two sections. The general medicinal chemistry guides the student through the general knowledge of drug action. The systematic section analyses in depth some drug classes of therapeutic intervention, with focus on the most recent drugs. The analysis of drug classes will be completed later by the “Chimica farmaceutica e tossicologica II” subject.
• General medicinal chemistry
Aim of the subject is to acquire knowledge of systematic naming of drugs, drug design and development and their catogerization, phamacokinetica and pharmacodinamica, mechanism of action, metabolism and toxicity.
• Systematic medicinal chemistry
Then, each drug class is analysed for the mechanism of action at molecular level, the structure-activity relationships, the metabolism and the synthesis of selected drugs.
Sulphamidics, quinolones, nitrofurans and nitroimidazoles
• Antibiotics petidoglycan synthesis inhibitors. Penicillins, cephalosporins, carbapenams
• Antibiotics inhibitors of ribosom. Aminoglycosides, macrolides, tetracyclins, chlororamfenicol, ansamicyns
• Other antibiotics
• Antimycobacterial agents
• Antifungal agents
• Antiparasitic agents
• Antiviral agents and AIDS treatment
• Cancer and chemotherapy
• Antiinfective agents
• Expectorant and mucolytic agents
• Tensioactive agents
• Gastrointestinal agents. Antiacid agents, antiulcer agents and purging agents

Adopted texts

Greco Giovanni. Farmacocinetica e farmacodinamica su basi chimico-fisiche. Ed. Loghìa
Greco Giovanni. Farmacoci antibatterici. II Ed. Loghìa
David A. Williams, Thomas L. Lemke, Foye’s principi di chimica farmaceutica. VII ed, Piccin Ed. (An English version of this book is available)
David A. Williams, Thomas L. Lemke, Foye’s L’essenziale. Piccin Ed. (An English version of this book is available)
A. Gasco, F. Gualtieri, C. Melchiorre, Chimica Farmaceutica, II Ed, CEA Ed.
E. Stevens, Chimica farmaceutica, Ed. Piccin (An English version of this book is available)
Files downloaded from the e-learning website

Bibliography

References of the teaching books.

Prerequisites

Organic chemistry and Microbiology

Frequency modes

Mandatory

Exam modes

Oral exam face-to-face or on-line

Programme

The subject “Medicinal and Toxicological Chemistry I” leads the student to acquire the basis of knowledge to understand the therapeutic action of the drug at chemical level. At the end of this subject, the student can understand the sequence of events inside the human body starting from the drug administration to its excretion. For a fruitful learning, this subject was shared into two sections, the general and the systematic action. The general medicinal chemistry leads the student through the general knowledge of drug action. The systematic section analyses in depth some drug classes generally used as pharmaceutical agents, mainly focused on the most recent drugs. The analysis of the drug classes will be completed later through the “Chimica Farmaceutica e Tossicologica II” subject.

GENERAL MEDICINAL CHEMISTRY (18 h)
Aim of the subject is to acquire knowledge of systematic naming of drugs, drug design and development and their categorization, pharmacokinetic and pharmacodynamics, mechanism of action, metabolism and toxicity.
For this part the book 1 and the file in elearning2 are suggested.

SYSTEMATIC MEDICINAL CHEMISTRY (70 h)
Each drug class is analysed with a particular focus on the mechanism of action at molecular level, the structure-activity relationships, the metabolism and the synthesis of selected drugs.
For this part the one of the books 2-5 and the files in elearning2 are suggested.


INORGANIC ANTISEPTIC DRUGS: (2 h)
For this part the files in elearning2 are suggested.

CHEMIOTERAPICS: (48 h)

Sulphamidics, quinolones, nitrofurans and nitroimidazoles
Antibiotics petidoglycan synthesis inhibitors and ribosom inhibitors
• Penicillins, cephalosporins, carbapenams, monobactams
• Antibiotics inhibitors of ribosom. Aminoglycosides, macrolides, tetracyclins, chlororamfenicol, ansamicyns
• Other antibiotics
• Antimycobacterial agents
• Antifungal agents
• Antiviral agents and AIDS treatment (8 h)
For this part the one of the books 2 and the files in elearning2 are suggested.


CANCER AND CHEMOTHERAPY (16 h)
For this part the one of the books 3-5 and the files in elearning2 are suggested.


ANTIULCER DRUGS (4 h)
For this part the one of the books 3-5 and the file in elearning2 are suggested.

See also: https://elearning.uniroma1.it/course/view.php?id=852

Adopted texts

1. Greco Giovanni. Farmacocinetica e farmacodinamica su basi chimico-fisiche. Ed. Loghìa
2. Greco Giovanni. Farmacoci antibatterici. Ed. Loghìa
3. David A. Williams, Thomas L. Lemke, Foye’s principi di chimica farmaceutica. 6° ed, Piccin Ed.
4. David A. Williams, Thomas L. Lemke, Foye’s L’essenziale. Piccin Ed.
5. John M. Beale, Jr, John H. Block. Wilson & Givolds Chimica farmaceutica, 1a Ed. italiana, Casa Ed. Ambrosiana
6. A. Gasco, F. Gualtieri, C. Melchiorre, Chimica Farmaceutica, 1a Ed, CEA Ed. (esce il 9 marzo).
7. E. Stevens, Chimica farmaceutica, Ed. Piccin.
8. File del materiale didattico su elearning2 (https://elearning.uniroma1.it/course/view.php?id=852)

Prerequisites

In view of a fruitful and enjoyable learning, at the beginning of the lessons the student must have proper knowledge of Organic Chemistry, in particular regarding the organic reactions and their mechanisms. Moreover, the student must know the 5, 6 and benzofused heterocycle naming and chemistry. The knowledge of Phisiology and Biochemistry is very important, in particular regarding the cell replication, the protein synthesis, the structure and DNA synthesis, the bacterial cell wall biosynthesis and viral replication. The knowledge of Microbiology mainly concerning the structure of infective agents, such as bacteria, viruses, fungi, plasmodia, mycobacteria, amoeba etc., is considered useful.

Exam modes

The subject “Chimica Farmaceutica e Tossicologica I” consists in lectures in lecture rooms. Each part can be depth using new or revised learning books. The teacher shows the student the suitable chapters for each of them. Moreover, files of the lessons can be downloaded from the e-learning website. The student can ask the teacher additional explanation on appointment. Lesson attendance is mandatory. Attendance aims to improve the quality of learning and to give a track record for the exam. Students who cannot attend the lessons, can download the detailed program and the teaching materials from the e-learning website, and receive assistance from the teacher