Anna Maria D'URSI | MEDICINAL CHEMISTRY I
Anna Maria D'URSI MEDICINAL CHEMISTRY I
cod. 0760200018
MEDICINAL CHEMISTRY I
| 0760200018 | |
| DIPARTIMENTO DI FARMACIA | |
| EQF7 | |
| PHARMACEUTICAL CHEMISTRY AND TECHNOLOGY | |
| 2023/2024 |
| OBBLIGATORIO | |
| YEAR OF COURSE 3 | |
| YEAR OF DIDACTIC SYSTEM 2020 | |
| SPRING SEMESTER |
| SSD | CFU | HOURS | ACTIVITY | |
|---|---|---|---|---|
| CHIM/08 | 9 | 72 | 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 GENERAL MEDICINAL CHEMISTRY, THE COURSE DEALS WITH THE STUDY OF ANTIMICROBIAL DRUGS ACTING AS ANTIBACTERIAL, ANTIMYCOBACTERIAL, ANTIFUNGAL, ANTIVIRAL, ANTICANCER, AND FINALLY ACTING, SUPPLEMENTING HORMONE AND VITAMIN ACTIONS 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 | |
|---|---|
| ADVANCED KNOWLEDGE OF ORGANIC CHEMISTRY, BIOCHEMISTRY MICROBIOLOGY, ANATOMY, PHYSIOLOGY, PATHOLOGY |
| Contents | |
|---|---|
| STRUCTURE, MECHANISM OF ACTION, STRUCTURE-ACTIVITY RELATIONSHIP, PHARMACOKINETICS AND PHARMACODYNAMICS, SYNTHESIS OF COMPOUNDS SELECTED FOR THE FOLLOWING THERAPEUTIC CLASSES: ANTIBACTERIALS FOR TOPICAL USE (6 H) SYNTHETIC ANTIBACTERIAL FOR SYSTEMIC USE: SULFONAMIDES AND DRUGS THAT ACT ON THE SYNTHESIS OF FOLIC ACID (6H) ANTIBACTERIAL FLUOROQUINOLONE, NITROFURAN AND NITROIMIDAZOLES; OXAZOLIDINONES (8H). ANTIBIOTICS THAT INTERFERE WITH PROTEIN SYNTHESIS: MACROLIDES, LINCOSAMIDES; AMPHENICOLS, TETRACYCLINES, AMINOGLYCOSIDES (10H) ANTIBIOTICS ACTING ON THE CELL WALL SYNTHESIS: PENICILLINS AND CEPHALOSPORINS, BETA-LACTAMASE INHIBITORS (10H) FOSFOMYCIN AND CYCLOSERINE. GLYCOPEPTIDE ANTIBIOTICS AND POLYPEPTIDE ANSAMICINE (4H). ANTIMYCOBACTERIAL DRUGS: ANTI-TUBERCULOSIS AND LEPROSTATICS (4H) ANTIFUNGAL AGENTS: INHIBITORS OF THE SYNTHESIS OF ERGOSTEROL; ANTIFUNGAL ACTIVE ON THE FUNGAL CELL MEMBRANE: CANDINE, POLYMYXINS AND NIKKOMICINE; GRISEOFULVIN. (4H) ANTIPROTOZOAL DRUGS: QUINOLINE, ANTIMALARIAL AGENTS, ARTEMISININ DERIVATIVES. (4H) ANTIVIRAL DRUGS: ANTI-HERPES, ANTI-HEPATITIS, ANTI-HIV, ANTI-INFLUENZA. ANTICANCER DRUGS USED FOR THE SARS COV2 TREATMENT (10H) DRUGS: ANTICANCER TARGETING DNA AND RELATED ENZYMES; ANTIMETABOLITES: INHIBITORS OF FOLATE; ANTITUMOR NATURAL PRODUCTS; NEW GENERATION ANTICANCER DRUGS. (10H) SERM. ESTRO-PROGESTIN DRUGS.(4H) DRUGS FOR HELMINTHIASIS TREATMENT DEEPENING AND VERIFICATION WORK (10H) |
| Teaching Methods | |
|---|---|
| LECTURES, INTERACTIVE TEACHING, TUTORIALS |
| Verification of learning | |
|---|---|
| THE EXAM IS DESIGNED TO ASSESS THE STUDENT'S ABILITY TO LEARN THE PRINCIPLES RELATED TO THE CHEMICAL STRUCTURE, THE MECHANISM OF ACTION AND THE STRUCTURE ACTIVITY RELATIONSHIP OF ANTIBIOTIC DRUGS AND CHEMOTHERAPEUTICS. THE VOTE, EXPRESSED IN THIRTIETHS WITH POSSIBLE PRAISE, WILL DEPEND ON THE ACQUIRED MATURITY ON THE CONTENTS OF THE COURSE. IT CONSISTS OF A WRITTEN TEST PRELIMINARY TO AN ORAL INTERVIEW. THE WRITTEN TEST PROPOSES QUESTIONS RELATED TO THE STRUCTURE, THE SYNTHESIS (WHERE REQUIRED), THE MECHANISM OF ACTION, THE PHARMACODYNAMIC AND PHARMACOKINETIC ASPECTS OF SINGLE MOLECULES BELONGING TO THE DIFFERENT CLASSES OF ANTIBIOTICS AND CHEMOTHERAPEUTICS. THE QUESTIONS IN NUMBER FROM 6 TO 8 REQUIRE CONCISE ANSWERS AND TEND TO VERIFY THE LEARNING AND ACCURACY OF THE KNOWLEDGE OF THE INDIVIDUAL PARTS OF THE PROGRAM. THE EVALUATION OF THE WRITTEN TEST IS FORMULATED GIVING AN APPROPRIATE SCORE TO EVERY SINGLE QUESTION. AT LEAST 18 POINTS MUST BE REACHED TO ACCESS THE ORAL EXAM. THE ORAL TEST WILL CONSIST OF AN INTERVIEW IN WHICH THE GAPS EVENTUALLY FOUND IN THE WRITTEN TEST WILL BE FILLED FOR THE PURPOSES OF PRAISE, THE FOLLOWING WILL BE TAKEN INTO ACCOUNT: I) THE QUALITY OF THE EXPOSITION, IN TERMS OF THE USE OF APPROPRIATE SCIENTIFIC LANGUAGE, II) THE ABILITY TO CROSS-CORRELATION BETWEEN THE DIFFERENT TOPICS OF THE COURSE AND, WHERE POSSIBLE, WITH OTHER DISCIPLINES; III) THE AUTONOMY OF PROVEN JUDGMENT. DURING THE COURSE IT IS POSSIBLE TO CARRY OUT TWO PARTIAL TESTS, RESPECTIVELY AFTER HALF OF THE LESSONS AND AT THE END OF SEMESTER. EACH TEST WILL WEIGH 50% ON THE FINAL MARK. THE EVALUATION OF THE TWO TESTS WILL BE EXPRESSED IN THIRTIETHS AND THE FINAL SCORE WILL BE GIVEN BY THE WEIGHTED AVERAGE OF THE TWO TESTS. IF THE FINAL SCORE IS ABOVE 18/30, STUDENTS CAN BE CONSIDERED EXEMPT FROM THE WRITTEN TEST. THE EXEMPTION WILL BE VALID EXCLUSIVELY FOR THE EXAMINATION SESSION FOLLOWING THE ONE OF TEACHING. |
| Texts | |
|---|---|
AN INTRODUCTION TO MEDICINAL CHEMISTRY (INGLESE) COPERTINA FLESSIBILE – 20113 DI GRAHAM L. PATRICK (AUTORE) COURSE MATERIAL (LESSON SLIDES, INSIGHTS ETC.) WILL BE PROVIDED TO STUDENTS AT THE END OF EVERY LESSON. THOMAS L. LEMKE, DAVID A. WILLIAMS FOYE - FOYE’S PRINCIPI DI CHIMICA FARMACEUTICA- PICCIN •GRECO GIOVANNI FARMACI ANTIBATTERICI - LOGHIA COURSE MATERIALS |
| More Information | |
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