Gianluca SBARDELLA | MEDICINAL AND TOXICOLOGICAL CHEMISTRY II
Gianluca SBARDELLA MEDICINAL AND TOXICOLOGICAL CHEMISTRY II
cod. 0760400022
MEDICINAL AND TOXICOLOGICAL CHEMISTRY II
| 0760400022 | |
| DIPARTIMENTO DI FARMACIA | |
| EQF7 | |
| PHARMACEUTICAL CHEMISTRY AND TECHNOLOGY | |
| 2024/2025 |
| OBBLIGATORIO | |
| YEAR OF COURSE 4 | |
| YEAR OF DIDACTIC SYSTEM 2023 | |
| SPRING SEMESTER |
| SSD | CFU | HOURS | ACTIVITY | |
|---|---|---|---|---|
| CHIM/08 | 12 | 96 | LESSONS |
| Objectives | |
|---|---|
| THE COURSE AIMS TO PROVIDE A RATIONAL APPROACH TO UNDERSTANDING THE ACTIVITY OF DRUGS AND THEIR DESIGN. THE PARTICIPANTS AT THE END OF THE COURSE WILL BE ABLE TO UNDERSTAND THE RELATIONSHIPS THAT LINK THE CHEMICAL STRUCTURE OF A DRUG TO ITS PHARMACOLOGICAL ACTIVITY THROUGH THE STUDY OF THE PHYSICO-CHEMICAL AND STEREO-ELECTRONIC PROPERTIES, AND OF THE MECHANISM OF ACTION. THE AIM OF THE COURSE IS ALSO THE STUDY OF THE MAIN CHEMICAL-PHARMACEUTICAL STRATEGIES USEFUL FOR THE OPTIMIZATION OF THE PHARMACODYNAMIC AND PHARMACOKINETIC PROPERTIES OF DRUGS. IN PARTICULAR, STARTING FROM THE KNOWLEDGE ACQUIRED IN THE COURSE OF MEDICINAL AND TOXICOLOGICAL CHEMISTRY 1, THE COURSE DEALS WITH THE STUDY OF DRUGS ACTING ON DIFFERENT SYSTEMS (CENTRAL NERVOUS SYSTEM, AUTONOMIC NERVOUS SYSTEM, CARDIOVASCULAR SYSTEM, GASTROINTESTINAL SYSTEM, ENDOCRINE AND METABOLIC DISORDERS). KNOWLEDGE AND UNDERSTANDING BY THE END OF THE COURSE THE STUDENT WILL KNOW: - THE MAIN REPRESENTATIVE DRUGS OF EACH CLASS STUDIED AND THE MAIN STEPS THROUGH WHICH THE CLASS WAS DEVELOPED - THE STRUCTURE-ACTIVITY RELATIONSHIPS OF SUCH DRUGS, THEIR MOLECULAR MECHANISM OF ACTION AND THEIR THERAPEUTIC CLASSIFICATION - SYNTHETIC PATHWAYS OF THE MOST REPRESENTATIVE COMPOUNDS OF EACH CLASS WILL ALSO BE DISCUSSED IN DETAILS, IN PARTICULAR THOSE EMPLOYED FOR THE INDUSTRIAL PREPARATION. APPLYING KNOWLEDGE AND UNDERSTANDING BY THE END OF THE COURSE THE STUDENT WILL BE ABLE TO: - CORRECTLY FRAME EACH MOLECULE STUDIED FROM THE POINT OF VIEW OF THERAPEUTIC APPLICATION AND MECHANISM OF ACTION, IDENTIFY THE ESSENTIAL PHARMACOPHORE AND ITS MODE OF INTERACTION WITH THE TARGET, IF KNOWN, AND COMMENT THE STRUCTURE-ACTIVITY RELATIONSHIPS; - ANALYZE POSSIBLE PK/PD ISSUES AND POSSIBLE STRUCTURAL MODIFICATIONS THAT COULD LEAD TO IMPROVED THERAPEUTIC PROFILE; - APPROPRIATELY DISCUSS IN DETAILS THE VARIOUS STEPS OF THE SYNTHESIS OF THE MOST REPRESENTATIVE COMPOUNDS OF EACH CLASS OF DRUGS. MAKING JUDGMENTS: THE STUDENT WILL BE ABLE TO: - PUT IN THE RIGHT CONTEXT THE QUESTIONS SHE/HE WILL BE ASKED DURING THE EXAMINATION (BOTH WRITTEN AND ORAL) AND SELECT THE MOST APPROPRIATE AND SPECIFIC ANSWER, AVOIDING UNNECESSARY AND NOT REQUESTED GENERAL DISSERTATIONS; - PROPERLY LINK TOGETHER THE KNOWLEDGE DERIVING FROM DIFFERENT DISCIPLINES ON A CERTAIN TOPIC AND INTEGRATE THEM TO HAVE A BETTER UNDERSTANDING. COMMUNICATION SKILLS: THE STUDENT WILL BE ABLE TO: - EXPLAIN AND DEVELOP CONCEPTS WITH CLARITY, SYNTHESIS AND LANGUAGE SKILLS. |
| Prerequisites | |
|---|---|
| IN ADDITION TO ALL THE COURSES OF THE 2ND YEAR, IT IS ALSO REQUIRED TO KNOW THE BASICS OF INTRODUCTIVE MEDICINAL CHEMISTRY, MEDICINAL CHEMISTRY I. |
| Contents | |
|---|---|
| INTRODUCTION TO MEDICINAL CHEMISTRY: NEUROTRANSMITTERS, HORMONS, RECEPTORS, ENZYMES (5 H) CHOLINERGIC TRANSMISSION AND CHOLINERGIC DRUGS (6 H) ADRENERGIC TRANSMISSION AND ADRENERGIC DRUGS (6 H) GENERAL ANAESTHETICS (2 H) LOCAL ANAESTHETICS (2 H) HYPNOTICS AND SEDATIVES (5 H) ANTICONVULSANT DRUGS (3 H) NON-STEROIDAL ANTI-INFLAMMATORY DRUGS (4 H) ANTIRHEUMATIC DRUGS AND DRUGS FOR THE TREATMENT OF ARTHRITIS, OSTEOARTHRITIS, AND GOUT (2 H) STEROID HORMONES (4 H) OPIOIDS (5 H) ENDOCANNABINOID SYSTEM (3 H) DRUGS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES (4 H) ANTIDEPRESSANT DRUGS (4 H) HALLUCINOGENS, PSYCHOACTIVE DRUGS, AND RECREATIONAL DRUGS (3 H) DRUGS FOR THE TREATMENT OF HEART FAILURE (4 H) ANTIANGINAL DRUGS (3 H) ANTIARRHYTHMIC AGENTS (2 H) ANTITHROMBOTIC DRUGS (ANTICOAGULANTS, ANTIPLATELET DRUGS, THROMBOLYTIC DRUGS) (4 H) ANTIHYPERTENSIVES (4 H) DIURETICS (3 H) ANTIHISTAMINES (2 H) DRUGS FOR ACID-RELATED DISORDERS (2 H) ANTIHYPERLIPIDEMIC AGENTS (4 H) HYPOGLYCEMIC AGENTS (4 H) DRUGS FOR THE TREATMENT OF OSTEOPOROSIS (2 H) |
| Teaching Methods | |
|---|---|
| THE COURSE WILL INCLUDE LECTURES AND IN-CLASS DISCUSSIONS OF PRIMARY LITERATURE FOR A TOTAL OF 96 HOURS (12 CFU = 12 ECTS). |
| Verification of learning | |
|---|---|
| THE FINAL EXAMINATION WILL CONSIST OF TWO PARTS: A ONE-HOUR WRITTEN EXAMINATION CONSISTING OF 3 EXERCISES (10 POINT EACH) EACH ONE CONTAINING QUESTIONS RELATED TO ONE OF THE TOPICS TAUGHT DURING THE COURSE; AND AN ORAL EXAMINATION CONSISTING OF IN-DEPTH QUESTIONS AND DISCUSSION OF THE TOPICS COVERED DURING THE COURSE. TO BE ADMITTED TO THE ORAL PART, THE STUDENT SHOULD DEMONSTRATE KNOWLEDGE OF THE TOPICS OF ALL THREE EXERCISES AND OBTAIN A SCORE OF AT LEAST 18/30. TEXTBOOKS, HANDOUTS, STUDENT'S OWN NOTES AS WELL AS ELECTRONIC DEVICES SUCH AS LAPTOPS, TABLETS OR SMARTPHONES ARE NOT PERMITTED DURING THE EXAMINATION. TO PASS THE EXAMINATION, BOTH PARTS MUST BE SUFFICIENT (MARK 18/30); THE FINAL MARK IS THE ARITHMETIC MEAN OF THE TWO MARKS. |
| Texts | |
|---|---|
| CHIMICA FARMACEUTICA, A CURA DI ALBERTO GASCO, FULVIO GUALTIERI, CARLO MELCHIORRE, ZANICHELLI. G.L. PATRICK, CHIMICA FARMACEUTICA, A CURA DI GABRIELE COSTANTINO, EDISES. G.L. PATRICK, INTRODUZIONE ALLA CHIMICA FARMACEUTICA, EDISES, II EDIZIONE. D.A. WILLIAMS, T.L. LEMKE, FOYE’S PRINCIPI DI CHIMICA FARMACEUTICA, PICCIN. 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, HTTP://PUBS.ACS.ORG/JOURNAL/JMCMAR CHEMMEDCHEM, HTTP://ONLINELIBRARY.WILEY.COM/JOURNAL/10.1002/(ISSN)1860-7187 NATURE REVIEWS DRUG DISCOVERY, HTTP://WWW.NATURE.COM/NRD/INDEX.HTML |
| More Information | |
|---|---|
| FOR MORE INFORMATION, PLEASE CONTACT PROF. GIANLUCA SBARDELLA (GSBARDELLA@UNISA.IT) OR VISIT THE WEBSITE HTTP://DOCENTI.UNISA.IT/005059 |
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