MEDICINAL CHEMISTRY I

Marina SALA MEDICINAL CHEMISTRY I

0760300013
DIPARTIMENTO DI FARMACIA
EQF7
PHARMACY
2024/2025

OBBLIGATORIO
YEAR OF COURSE 3
YEAR OF DIDACTIC SYSTEM 2023
SPRING SEMESTER
CFUHOURSACTIVITY
1080LESSONS
Objectives
MEDICINAL CHEMISTRY I-CHIM/0810BTHE COURSE IS AIMED AT THE ACQUISITION OF KNOWLEDGE AND UNDERSTANDING OF THE VARIOUS STAGES OF SYNTHESIS, CHEMICAL-PHYSICAL CHARACTERISTICS AND THE RELATIONSHIP BETWEEN THE STRUCTURE AND BIOLOGICAL ACTIVITY OF ANTI-INFECTIOUS AND ANTICANCER DRUGS.

AT THE END OF THE COURSE THE STUDENT WILL KNOW:
THE STAGES OF SYNTHESIS, PHYSICAL AND CHEMICAL PROPERTIES, MECHANISMS OF ACTION AND USES OF ANTIBIOTICS, ANTICANCER, ANTIFUNGAL, ANTISEPTIC, DISINFECTANT, ANTIVIRAL AND ANTIMALARIAL.

THE STUDENT APPLYING THE ACQUIRED SKILLS MUST BE ABLE TO:
-INTERPRET AND ANALYSE THE STRUCTURE OF DRUGS AND THEIR PHARMACOLOGICAL ACTIVITY, AND THE STEPS THAT GOVERN RESEARCH IN THE CHEMICAL-PHARMACEUTICAL FIELD FROM THE DISCOVERY OF LEAD COMPOUNDS TO MARKETING.
Prerequisites
ACQUISITION REQUIRED FOR THE FOLLOWING DISCIPLINES: ORGANIC CHEMISTRY
Contents
DEFINITION OF DRUG; THE ACTIVE INGREDIENT AND PHARMACEUTICAL FORMS. DRUG DISCOVERY; THE MODERN TECHNOLOGIES IN DISCOVERY AND DRUG DEVELOPMENT. DRUGS FROM NATURAL AND SYNTHETIC ORIGIN. PHYSICO-CHEMICAL PROPERTIES OF DRUGS. PHARMACOKINETICS ; INTERACTIONS AMONG DRUGS AND AMONG DRUGS AND FOODS. BIOAVAILABILITY AND BIOEQUIVALENCE (8 H).
GENERIC DRUG. PHARMACODYNAMICS. AGONISTS, ANTAGONISTS, PARTIAL AGONISTS AND INVERSE AGONISTS. DRUG-METABOLIC INDUCTION AND INHIBITION. ENZYME INHIBITION. DRUGS CLASSIFICATION INFLUENCE OF ISOMERISM ( OPTICAL , GEOMETRICAL AND CONFORMATIONAL) ON THE PHARMACOLOGICAL ACTIVITY. ROUTES OF ADMINISTRATION AND EXCRETION (8H).
SPECIAL SECTION: ANTISEPTICS AND DISINFECTANTS (2H).
SISTEMIC ANTIBIOTICS: SULFONAMIDES AND DRUGS ACTING ON FOLIC ACID SYNTHESIS; FLUOROQUINOLONIC DRUGS, NITROFURANIC, NITROIMIDAZOLIC AND OXAZOLIDINDIONIC DRUGS; ANTIBIOTIC INTERFERING WITH PROTEIC SYNTHESIS: MACROLIDS, LINCOSAMIDES, AMFENICOLS, TETRACYCLINE, AMINOGLYCOSIDES. ANTIBIOTICS INTERFERING WITH CELL WALL SYNTHESIS: PENICILLINS, CEPHALOSPORINS, BETALATTAMASES INHIBITORS, PHOSPHOMYCIN AND CYCLOSERINE; GLICOPEPTIDIC AND POLIPEPTIDIC DRUGS, ANSAMYCINES (14 H).
ANTIMYCOBACTERIC DRUGS: ANTILEPROSY AND ANTITUBERCOLAR DRUGS (4H);
ANTIFUNGAL DRUGS: INHIBITORS OF ERGOSTEROL SYNTHESIS, AZOLIC AND ALLYLAMINIC DRUGS, ANTIFUNGAL ACTING ON CELL MEMBRANE: CANDIN, POLIMIXIN AND NIKKOMICIN; GRISEOFULVIN (4H).
ANTIPROTOZOIC DRUGS: QUINOLONIC ANTIMALARIAL, ANTIMETABOLITES AND ARTEMISININ DERIVATIVES (2H).
ANTIVIRAL DRUGS: ANTIHIV, ANTI HEPATITIS B AND C, ANTICORONAVIRUS AGENTS (10H).
ANTICANCER DRUGS ACTING ON DNA AND CORRELATED ENZYMES, ANTIMETABOLITES, FOLATE INHIBITORS, PURINIC AND PYRIMIDINIC ANALOGUES, NATURAL ANTITUMOR DRUGS, LAST GENERATION DRUGS (16H).
SYNTHESIS OF PRINCIPAL DRUGS BELONGING TO DISCUSSED CLASSES (12 H).
Teaching Methods
80 HOURS OF CLASSROOM LESSONS ARE PROVIDED ON ALL THE SUBJECTS OF THE COURSE.
Verification of learning
ACHIEVEMENT OF THE OBJECTIVES IS CERTIFIED BY PASSING AN EXAM.THE EXAM PROVIDES FOR A PRELIMINARY WRITTEN EXAM TO AN ORAL EXAM SCHEDULATED ON DIFFERENT DAYS. THE WRITTEN TEST CONSISTS OF FIVE ANSWER AND IT HAS A DURATION NOT EXCEEDING 150 MINUTES AND IS AIMED AT VERIFYING THE ABILITY TO PROPERLY APPLY THEORETICAL KNOWLEDGE AND THE ABILITY TO COMMUNICATE IN WRITING. THE ORAL TEST CONSISTS OF A 20-MINUTE DISCUSSION AIMED AT ASSESSING THE LEVEL OF KNOWLEDGE AND UNDERSTANDING ACQUIRED BY THE STUDENT ON THE THEORETICAL CONTENTS OF THE PROGRAM. THE ORAL TEST WILL ALSO ALLOW STUDENTS TO COMMUNICATE WITH THE LANGUAGE SKILLS AND AUTONOMOUS EXPOSURE ORGANIZATION ON THE SAME SUBJECTS WITH THEORETICAL CONTENT.
The final assessment will not be based solely on the calculation of the arithmetic mean of the scores obtained in the individual tests , but will take into account the assessments obtained in each test independently. A qualitative evaluation of the student’s overall performance will be carried out, taking into account various aspects such as the demonstrated knowledge, the quality of the work performed, problem-solving skills and other relevant elements.
Texts
D.A. WILLIAMS, T.L. LEMKE, FOYE’S PRINCIPI DI CHIMICA FARMACEUTICA, PICCIN.
• G.L. PATRICK, INTRODUZIONE ALLA CHIMICA FARMACEUTICA, EDISES, II EDIZIONE
• WILSON&GISVOLD CHIMICA FARMACEUTICA .ED.CEA
• T. NOGRADY, D. WEAVER, MEDICINAL CHEMISTRY – A MOLECULAR AND BIOCHEMICAL APPROACH, 3RD ED.,
OXFORD UNIVERSITY PRESS.
• MONOGRAFIE DELLA COLLANA "CHIMICA DEI RECETTORI", EDITORE C. MELCHIORRE, CLUEB (BOLOGNA).
• C. WERMUTH, LE APPLICAZIONI DELLA CHIMICA FARMACEUTICA, EDISES.
• P. KROGSGAARD-LARSEN, T. LILJEFORS, U. MADSEN ED., TEXTBOOK OF DRUG DESIGN AND DISCOVERY, TAYLOR
& FRANCIS.
• GOODMAN & GILMAN'S THE PHARMACOLOGICAL BASIS OF THERAPEUTICS, TWELFTH EDITION, MCGRAW-HILL
MEDICAL PUBLISHING DIVISION (2011).
• WILSON AND GISVOLD'S TEXTBOOK OF ORGANIC MEDICINAL AND PHARMACEUTICAL CHEMISTRY-LIPPINCOTT
WILLIAMS & WILKINS
• KLEEMANN, ENGEL, KUTSCHER, REICHERT, PHARMACEUTICAL SUBSTANCES, 5TH ED., THIEME VERLAG.
• BURGER’S MEDICINAL CHEMISTRY, DRUG DISCOVERY AND DEVELOPMENT. 7TH EDITION. WILEY. JOURNAL OF
MEDICINAL CHEMISTRY, ACS.
-ALBERTO GASCO FULVIO GUALTIERI CARLO MELCHIORRE
CHIMICA FARMACEUTICA, SECONDA EDIZIONE, 2020

More Information
THE COURSE IS TAUGHT IN ITALIAN
THE ATTENDANCE IS MANDATORY
LOCATION: DEPARTMENT OF PHARMACY
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