Learning outcome. The student should become able to appreciate the basic elements of the mode of action, chemical properties and metabolic transformation of the classes of drugs, or individual drugs, listed below. and be able to critically evaluate the information available on drug-drug interactions and side effects.

1. Drugs affecting the Cardiovascular system
1.1 Cardiac glycosides
1.2 Antianginal and antiarrhytmic drugs
1.3 Diuretics
1.4 Angiotensin enzyme inhibitors and Angiotensin II receptor AT1 antagonists
1.5 Calcium channel blockers
1.6 Central and peripheral sympatholytics and vasodilators
1.7 Centrally acting sympatholytic drugs ( methyldopa, clonidine, guanabenz, guanfacine)
1.8 Beta-Adrenergic blocking drugs
1.9 Alpha-Adrenergic blocking drugs
1.10 Mixed alpha/beta-adrenergic blocking drugs
1.11 Vasodilators
1.11.1 Arterial vasodilators (hydralazine, minoxidil, diazoxide)
1.11.2 Arterial and venous vasodilators (sodium nitroprusside)
1.12 Antihyperlipoproteinemics and inhibitors of cholesterol biosynthesis
1.13 Antithrombotics, thrombolytics and Coagulants
2. Drugs affecting the hormonal system
2.1 Insulin and oral hypoglycemic drugs
2.2 Estrogens, Progestins and Androgens
2.3 Thyroid hormones and thyroid drugs
3. Antiulcer drugs.
3.1 H2 receptor Antagonists
3.2 H+/K+-ATPase proton pump inhibitors
4. Chemotherapeutic Agents
4.1 Antibiotics and antimicrobials.
4.1.1 Sulfonamides
4.1.2 Trimethoprim
4.1.3 Quinolones
4.1.4 Phosphomycin
4.2 Inhibitors of bacterial cell wall biosynthesis
4.2.1 Penicillins and beta-lactamases irreversible inhibitors
4.2.2 Cephalosporins
4.2.3 Carbapenems
4.2.4 Monobactams
4.2.5 Vancomycin and Teichoplanin
4.2.6 Bacitracin
4.3 Inhibitors of protein biosynthesis
4.3.1 Aminoglycosides.
4.3.2 Macrolides
4.3.3 Teyracyclines
4.3.4 Chloramphenicol
4.3.5 Linezolid
4.4 Antiparasitic Agents
4.4.1 Nitroimidazoles and Nitrofurans
4.4.2 Pentamidine
4.4.3 Atovaquone
4.4.4 Antimalarial drugs
4.4.4.1 Quinine, 4- and 8- substituted quinolines
4.4.4.2 Pyrimethamine and Pyrimethamine-Sulphadoxine combination
4.4.4.3 Artemisinins
4.6 Antifungal drugs
4.6.1 Polyenes
4.6.2 Imidazoles and Triazoles
4.6.3 Allylamines
4.6.4 Morpholines
4.6.5 Echinocandine
4.6.6 Flucitosine, Griseofulvin, Haloprogin
4.7 Antimycobacterial agents
4.7.1 Anti-Tuberculosis
4.7.1.1 Capreomycin
4.7.1.2 Cycloserine
4.7.1.3 Ethanbutol
4.7.1.4 Isoniazide
4.7.1.5 Kanamycin
4.7.1.6 p-Aminosalicylic acid
4.7.1.7 Pyrazinamide
4.7.1.8 Rifampin
4.7.1.9 Rifapentine
4.7.1.10 anti-mycobacterium avium intracellulare (Azithromycin, Clarithromycin)
4.7.1.11 anti-Leprosy (Dapsone, Clofazimine, Thalidomide)
4.8 Antiviral agents and Protease inhibitors
4.8.1 Antiviral agents interfering with cellular penetration and early replication (Amantadine, Rimantadine, Zanamivir, Oseltamivir)
4.8.2 Agents interfering with viral nucleic acid replication (acyclovir, valacyclovir,Cidofovir, Cytarabine, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridin, Ribavirin, Trifluorothymidine, Vidarabine)
4.8.3 Antiretroviral agents and Protease Inhibitors (Zidovudine, Didanosine, Zalcitabine, Stavudine, Lamivudine, Abacavir, Nevirapine, Delavirdine, Efavirenz, Sequinavir, Ritonavir, Indinavir, Nelfinavir, Amprenavir, Lopinavir, Ritonavir)

Medicinal Chemistry I

The course is meant to make the studentsunderstand  the fundamental relationship between chemical structure of a drug and its interaction with biological targets. The course deals with the medicinal chemistry techniques that led to the discovery, optimization and proof of the mode of action of the treated drugs as well as their metabolites and when possible their anticipation. The students are expected to understand that the chemical structure of a drug and its rational modification are among the basic factors torationalize and improve the actions of any drug. The students are also expected to be able to integrate into a general method of evaluation the notions studied on the particular classes of drugs dealt with during the course and be able to independently and critically transfer these notions with a simple but technically correct language

The teaching material prepared by the lecturer in addition to recommended textbooks (such as for instance slides, lecture notes, exercises, bibliography) and communications from the lecturer specific to the course can be found inside the Moodle platform › blended.uniurb.it

The medicinal texts listed in the Course books section and the additional teaching material provided by the lecturer. The teaching material will be found inside the Moodle platform.

Teaching

frontal lessons in the italian language

Attendance

Attendance is recommended but is but not mandatoey. Students should have a sufficient knowledge of organic chemistry to  understand the chemical and metabolic behaviour of the drugs treated during the course. Knowledge of english sufficient to read and understand a brief scientific text related to the drugs that are being treated in the program

Course books

Required:

Foye's Principles of Medicinal Chemistry, T.L.Lemke, D.A.Williams editors, sixth edition., Lippincot, Williams and Wilkins 2008.

Essentials of Foyes Princuples of Medicinal Chemistry Wolters Kluwers Health Inc. 2017

Optional

J.M. Beale, Jr., J.M.Block, Wilson & Gisvold's Textbook of Organic and Pharmaceuticall Chemistry 12th edition, Lippincot, Williams & Wilkins 2011.

G. L. Patrick An Introduction to Medicinal Chemistry 5th edition, Oxford University Press 2013.

A. Gasco, F. Gualtieri, C. Melchiorre editors, Chimica Farmaceutica, Casa Editrice Ambrosiana 2015.

Assessment

The final exam consists of a preliminary written test followed by an oral interrogation and failure in any one of the two proofs implies repetition of both. The written test consists of ten open questions, relevant to drugs covered during the semester, and it must be completed within two hours: The interrogation on topics different from or in part coincident with those of the written test lasts 30-45 minutes. The scheme allows a uniform and thorough evaluation of the students knowledge and understanding of the topics treated during the semester.

Disability and Specific Learning Disorders (SLD)

Students who have registered their disability certification or SLD certification with the Inclusion and Right to Study Office can request to use conceptual maps (for keywords) during exams.

To this end, it is necessary to send the maps, two weeks before the exam date, to the course instructor, who will verify their compliance with the university guidelines and may request modifications.

Attendance

Same as for the attending students.

Course books

Same as for the attending students.

Assessment

Same as for the attending students.

Disability and Specific Learning Disorders (SLD)

Students who have registered their disability certification or SLD certification with the Inclusion and Right to Study Office can request to use conceptual maps (for keywords) during exams.

To this end, it is necessary to send the maps, two weeks before the exam date, to the course instructor, who will verify their compliance with the university guidelines and may request modifications.