MEDICINAL AND TOXICOLOGICAL CHEMISTRY 2

Università degli Studi
"G. d'Annunzio"

Chieti - Pescara

Single discipline educational activity

Course Sheet

Course code:

00204

Academic Year of enrolment:

2020

Year of supply:

2023/2024

Type of Course:

Characterising

Degree:

Course of Single Cycle Degree 5 years in PHARMACY

Disciplinary Sector:

Pharmaceutical Chemistry

Language:

Italian

Location:

CHIETI

Divisions:

Cognomi A-G - Professor: AMOROSO Rosa
Cognomi A-G - Professor: MACCALLINI Cristina
Cognomi H-Z - Professor: CARRADORI SIMONE

Credits:

Programme Year:

Cycle:

First semester

Obligatory attendance:

Yes

Minimum hours of attendance:

Hours of classroom activity:

100

Individual study hours:

200

Prerequisites:

The attendance of the “Medicinal Chemistry II” course foresees that the student has acquired, in his/her study path, the basic knowledge of Organic Chemistry, Biochemistry and Physiology and has dealt with in depth the study of the relationships between chemical-physical properties and drug activity.
The access to the exam is subject to passing the “Medicinal Chemistry I” exam

Objectives

The objective of “Medicinal Chemistry II” is the knowledge of the structures and mechanisms of action of the main chemotherapeutics, anticancer, hormones and hormone analogues currently used for humans, together with the deepening of the chemical-toxicological aspects and the study of structure-activity relationships

Contents

LESSONS
General section
Principles of catalysis, enzyme inhibition and metabolic antagonism
Chemotherapeutic agents and antibiotics
Antiseptics and disinfectants
Sulfonamides and dihydrofolate reductase inhibitors
β -lactam antibiotics: penicillins, cephalosporins, monobactams, carbapenems, β-lactamase inhibitors
Other antibiotics that interfere with the synthesis of peptidoglycan and the integrity of the bacterial membrane: glycopeptides, polypeptides and fosfomycin
Inhibitors of bacterial protein synthesis: macrolides, tetracyclines, aminoglucosides, chloramphenicol, oxazolidinones
Synthetic antibacterials: quinolones, metronidazole, methenamine, nitrofurantoin
Antimycobacterials: isoniazid, pyrazinamide, ansamycins
Antifungals: azoles, allyl amines, polyene antibiotics
Antimalarials: quinine and quinidine, mefloquine, aminoquinolines, antimetabolites, artemisinin
Antivirals: drugs against HIV, HSV, and influenza viruses. Coronaviruses.
Anticancer agents: cytotoxic alkylating agents, analogues of nucleosides, DNA intercalating agents, mitosis blockers, antibiotics, alkaloids, topoisomerases inhibitors; target therapy and immunotherapy
Hormones and hormone analogues
Biosynthesis of cholesterol and steroid hormones
Corticosteroids: natural and synthetic glucocorticoids and mineralocorticoids
Sex hormones: natural and synthetic estrogens, progestins, and androgens
Biosynthesis of prostaglandins, selective and nonselective NSAIDs
Hypothalamus and pituitary peptide hormones, insulin and oral hypoglycemic agents
Hormones of the thyroid
Calcium metabolism and related drugs

EXERCITATIONS
Insights of Lessons topics regarding: graphical representations and nomenclature assignment of selected molecules by using specific software; modulation of SAR and pharmacokinetic properties; bibliographic sources (scientific articles, patents, databases)

Extended Syllabus

Principles of catalysis, enzyme inhibition and metabolic antagonism
antiseptics and disinfectants
Chemotherapeutic agents
Sulfonamides and dihydrofolate reductase inhibitors
b-lactam antibiotics: penicillins, cephalosporins, monobactams, carbapenems, β-lactamase inhibitors
Other antibiotics that interfere with the synthesis of peptidoglycan and the integrity of the bacterial membrane: glycopeptides, polypeptides and fosfomycin
Inhibitors of bacterial protein synthesis: macrolides, tetracyclines, aminoglucosides, chloramphenicol, oxazolidinones
Synthetic antibacterials: quinolones, metronidazole, methenamine, nitrofurantoin
Antimycobacterials: isoniazid, pyrazinamide, ansamycins
Antifungals: azoles, allyl amines, polyene antibiotics
Antimalarials: quinine and quinidine, mefloquin, aminoquinolines, antimetabolites, artemisinin
Antivirals: drugs against HIV, HSV, and influenza viruses. Coronavirus
Anticancer agents: cytotoxic alkylating agents, analogues of nucleosides, DNA intercalating agents, mitosis blockers, antibiotics, alkaloids, topoisomerases inhibitors; target therapy and immunotherapy
Hormones and hormone analogues
Biosynthesis of cholesterol and steroid hormones
Corticosteroids: natural and synthetic glucocorticoids and mineralocorticoids
Sex hormones: natural and synthetic estrogens, progestogens and androgens
Biosynthesis of prostaglandins, non-steroidal anti-inflammatory drugs and selective COX2 inhibitors
Peptide hormones of the hypothalamus and pituitary gland, insulin and oral hypoglycemic agents
Thyroid hormones
Calcium metabolism and vitamin D-dependent hormones

Recommended Bibliography

Foye’s, Principi di Chimica Farmaceutica, Ed. Piccin
Gasco, Gualtieri, Melchiorre. Chimica Farmaceutica. 2° edizione, Casa Editrice Ambrosiana

Methods of Provision

Conventional

Teaching Methods

The course consists of 80 hours of lectures and 20 hours of exercises in the classroom with simulations of exam tests

Evaluation methods

Verification of learning:

The final exam consists in an oral interview, with the aim to check the knowledge and understanding of the issues related to the course program. a fundamental requirement of the examination is the knowledge of the chemical structure, structure-activity relationships and action mechanisms relating to the compounds covered by the program. The final evaluation is considered positive if the student, in addition to knowing the proposed topics, exposes them clearly and with appropriate terminology

Contacts/More Information

The publicity of lesson schedules and educational programs is ensured by the University and Department websites. The publication of exam sessions is assured by the ESSE3 application

Università degli Studi
"G. d'Annunzio"

Chieti - Pescara

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