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.

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 critically explain to the students 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 to understand 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 drugs dealt with in the course and be able to independently and critically transfer their conclusions 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 latest Italian translation of Foye's Principles of Medicinal Chemistry 7th edition or later

Teaching

frontal lessons

Course books

Foye's Principles of Medicinal Chemistry, T.L.Lemke, D.A.Williams editors, sixth edition., Lippincot, Williams and Wilkins 2008. The material will be integrated when necessary with articles taken from primary sources.

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 about 30 minutes. The scheme allows a uniform and thorough evaluation of the students knowledge and understanding of the topics treated during the semester.

Disabilità e DSA

Le studentesse e gli studenti che hanno registrato la certificazione di disabilità o la certificazione di DSA presso l'Ufficio Inclusione e diritto allo studio, possono chiedere di utilizzare le mappe concettuali (per parole chiave) durante la prova di esame.

A tal fine, è necessario inviare le mappe, due settimane prima dell’appello di esame, alla o al docente del corso, che ne verificherà la coerenza con le indicazioni delle linee guida di ateneo e potrà chiederne la modifica.