Catalogo dei Corsi di studio

General expected learning outcomes
The student will acquire the tools and theoretical-practical strategies for the discovery and design of new active ingredients; in particular, the student will understand the necessary steps from the identification of a molecular prototype to the optimization of a molecule to the realization of a drug.
He or she will, likewise, be able to apply the knowledge acquired in the professional field in the chemical-pharmaceutical industry. In addition, the student will be able to recognize the main chemical structures of drugs belonging to the classes covered in the "syllabus" and will have the ability to design the chemical synthesis of drugs and discuss their properties both qualitatively and quantitatively in terms of structure-activity relationships, physicochemical and pharmaco-toxicological properties.

Specific expected learning outcomes
1. Knowledge and understanding
The student will learn all aspects inherent in the history and molecular development of the classes of drugs with anti-infective activity (antibiotics, antivirals, antifungals, antiparasitics), gastro-intestinal dysfunctions (anti-ulcer, anti-diarrheals, antihistapsi, antacids) and antitumor, with particular reference to the molecular mechanisms of biochemical-biological action, their chemical-pharmaceutical, pharmacological and toxicological properties. Furthermore, the student will know the etiopathogenetic mechanisms that cause the various diseases object of therapeutic treatments with the studied drugs.

2. Applying knowledge and understanding
At the end of the course, the student will be able to identify the different structures of drugs, analyze their biological, pharmacological and toxicological mechanisms of action, and most importantly, be able to adopt strategies for both structural and chemical synthesis design for the eventual development of new chemicals to be transformed into drugs.
Knowledge of the methodologies for the identification and optimization of the parent compounds (lead compounds) will enable the student to be able to approach in academic and/or industrial settings the discovery and/or practical development of new chemical entities, to be able to improve both their pharmacological-therapeutic and toxicological profiles, which are important to achieve market introduction of new drugs. Knowledge of the most prevalent therapeutic problems and pharmaceutical solutions available in the treatment of the diseases discussed in the "syllabus" will make the student proficient and intuitive in the rational choice/consideration of such drugs in the field of human health.

3. Making judgements
The lecturer will stimulate students to develop a logical-critical sense by asking frequent questions (brainstorming) during the lecture with the aim of inducing them to acquire skills in linking (correlative thinking) between the various concepts defined in the "syllabus," mastering the subject matter, but also to consider the study of pharmaceutical and toxicological chemistry I as an integral part and link with other disciplines already studied (anatomy, biology, organic chemistry, molecular biology, microbiology, biochemistry, physiology, pathology) and with others that will follow in future training (pharmaceutical and toxicological chemistry II, pharmacology, pharmacognosy, toxicology, pharmaceutical techniques and legislation, chemical and physical methods in organic chemistry). The instructor will periodically ask students to develop in-depth treatises/theses pertaining to key topics discussed in class, to habituate them to the design of chemical-pharmaceutical scientific research, will submit the students to learning tests to allow for their self-assessment and to have feedback on the teacher's teaching method. At the end of the course, students will be able to make analytical/critical judgment, interpret and correlate complex concepts, and design research inherent in the topics covered for the purpose of expanding scientific, ethical and social knowledge.

4. Communication skills
Through the acquisition of knowledge and understanding, the ability to apply them and to propose a critical judgment on the topics covered, but also through the aid of the related scientific language used by the lecturer during the course and the frequent stimulation of communication of what has been learned in class, the student will be able to communicate with cognitive and linguistic-perceptual depth with figures who are his or her peers and/or who belong to an inherent scientific and social community or of a different cultural background.

5. Learning skills
The student who has acquired the skills described above will be able to undertake future studies in the pharmaceutical field in a more autonomous, self-directed and rapid manner, but also to propose in social and/or work contexts issues useful to the scientific progress of society in the field of human health.

Programme

Program Carried Out Detailed in AA 2021-2022 and will be updated for AA 2022-2023.
[N] indicates that only the name is to be given
[S] indicates that one should study the synthesis
IMPORTANT!!!: where the synthesis of a drug is indicated the choice of one or more examples must involve a different structure. In any case, the student should at least be able to name most of the drug names for each group of substances given in the various chapters.

1 Organic Chemistry and Biochemistry for Pharmaceutical Chemistry>
1.1 Recognition of Functional Groups from 2D and 3D Structures
1.2 Recognition of Amino Acids and Azide Bases from 2D and 3D Structures
1.3 Recognition of Sugars from 2D and 3D Structures
1.4 Recognition of Mixed 2D and 3D Structures
1.5 Representation of Organic Molecules in 1D, 2D and 3D
1.5.1 File Formats of Molecules
1.5.2 Drawing of Organic Molecules
1.5.2.1 JchemPaint
1.5.2.2 JSME
1.5.2.3 Marvin Sketch
1.5.3 Simplified Molecular-Input Line-Entry System (SMILES) (1D)
1.5.4 International Chemical Identifier (1D)
1.5.5 sdf (2D and 3D)
1.5.6 pdb (3D biomolecules)
1.5.7 mol2 (3D organic molecules)
1.5.8 Interconversion of file formats
1.6 Representation of Macromolecules in 1D, 2D and 3D
1.6.1 Web Applications (Protein Data Bank -PDB)
1.6.2 UCSF Chimera
2 Introduction to Pharmaceutical Chemistry
2.1 Definitions.
2.1.1 Medication (Ita)
2.1.2 Medication (Eng)
2.2 History
2.3 Scope of Pharmaceutical Chemistry and Pharmaceutical Chemist
2.4 Origin of Drugs
2.4.1 Medications of Natural Origin
2.4.2 Drugs of Semisynthesis
2.4.3 Drugs of Synthesis
2.4.4 Parallel and combinatorial synthesis
3 Macromolecules of Pharmaceutical Chemical Interest.
3.1 Definition.
3.1.1 Importance of knowing the targets
3.1.2 How many targets?
3.1.3 Omics
3.2 Proteins
3.3 Nucleic Acids
3.4 Carbohydrates
3.5 BigSMILES
3.6 Visualization of Macromolecules
4 Pharmaceutical Phases
4.1 Definitions.
4.1.1 Pharmaceutical Phase
4.1.2 Pharmacokinetic Phase
4.1.3 Pharmacodynamic Phase
4.2 Pharmacokinetic Phase
4.2.1 ADME, LADME, ADMET, and LADMET
4.2.1.1 Drug routes of administration
4.2.1.2 Absorption of Drugs
4.2.1.3 Distribution of Drugs
4.2.1.4 Metabolism of Drugs
4.2.1.5 Elimination of Drugs
4.3 Details of Drug Metabolism
4.3.1 Phase I Reactions
4.3.1.1 Cytochromes P450:
Classification and Nomenclature
Role in drug metabolism
Polymorphism
Role in Toxicity
Oxidative Cycle
Reactions
Metabolic Activation
Inhibition and Activation of P450
Reactions without P450 involvement
4.3.2 Phase II Reactions
4.3.2.1 Glucuronation
4.3.2.2 Sulfoconjugation
4.3.2.3 Glutathionylation
4.3.2.4 Acetylation and methylation
4.3.2.5 Hippuric Conjugation
4.3.3 First Passage Effect
4.3.4 Metabolic Stability
4.3.5 Propharmaceuticals and Derivatives
4.4 Properties of Drugs in Pharmacokinetics
4.4.1 Lipophilicity and Hydrophilicity (logP and logD)
4.4.2 pKa
4.4.3 Solubility
4.4.4 Rule of 5, Variants and Drug Likeness
4.4.4.1 Lipinsky (Rule of 5)
4.4.4.2 Veber
4.4.4.3 Ghose
4.4.4.4 Congreve (Rule of 3)
4.4.5 Drug-Like Properties
4.5 Prediction of Parameters and Pharmacokinetic Profiles.
4.5.1 Software
4.5.2 Web Applications
4.6 Pharmacodynamic Phase
4.6.1 Drug/Macromolecule Interactions.
4.6.1.1 Types of Interactions
4.6.1.1.1 Covalent Bonds
4.6.1.1.2 Ionic Bonds
4.6.1.1.3 Ion-Dipole and Dipole-Dipole Bonds
4.6.1.1.4 Hydrogen Bonds
4.6.1.1.5 Charge Transfer Bonds
4.6.1.1.6 Hydrophobic Interactions
4.6.1.1.7 Cation-Pi Interactions
4.6.1.1.8 Halogen Bonding
4.6.1.1.9 London (van der Waals) dispersion forces
4.6.1.1.10 Typical Non-Bonding Distances
4.6.1.2 Numerical Determination of Interactions
4.6.1.2.1 Steric Interactions
4.6.1.2.2 Electrostatic Interactions
4.6.1.3 Molecular Interaction Fields (MIFs)
4.6.2 Expression of Potency of a Drug
4.6.2.1 IC50/EC50/Ki/LD50
4.6.2.2 Efficiency (LE), Lipophilic Efficiency(LiPE) of a Ligand and Maximum Affinity of Ligands
4.6.3 Binding Mode (Binding Mode)
4.6.3.1 Lock/Key Theory
4.6.3.2 Induced Adaptation Theory
4.6.3.3 Theory of Conformational Selection (HIV RT/Pr)
4.6.4 Ligands and Types of Ligands
4.6.4.1 Ligands
4.6.4.2 Ligands of Enzymes
4.6.4.2.1 Enzyme Inhibitors
4.6.4.2.1.1 Irreversible Inhibitors
4.6.4.2.1.2 Reversible Inhibitors
4.6.4.2.1.2.1 Competitive
4.6.4.2.1.2.2 Acompetitive
4.6.4.2.1.2.3 Noncompetitive
4.6.4.2.1.2.4 Mixed Inhibitors
4.6.4.2.2 Enzyme Activators
4.6.4.3 Receptor Ligands
4.6.4.3.1 Agonists
4.6.4.3.2 Antagonists
4.6.4.3.3 Inverse Agonists
4.6.4.4 Proteolysis Targeting Chimera (PROTAC - New Frontiers)
5 Drug Discovery and Drug Invention (Drug Discovery and Drug Design)
5.1 Introduction.
5.1.1 General Information on Drug Discovery and Invention
5.2 Hits, Hits to Lead, Leads
5.2.1 Hits
5.2.2.Databases
5.2.1.1 ZINC
5.2.2.2 ChEMBL
5.2.2.3 PubChem
5.2.2.4 Binding DB
5.2.2.5 DrugBank
5.2.2.6 Re-Frame DB
5.2.3 Hits to Leads
5.2.4 Lead Compounds
5.2.5 Lead Optimization (Drug-Like Compounds)
5.3 Analogues
5.3.1 Types of Analogs
5.3.2 Chemical Description
5.3.2.1 Molecular Descriptors
5.3.2.2 The Method of Topliss
5.3.3 Structural Description
5.3.3.1 Molecular Fingerprints
5.3.4 Molecular Similarity
5.3.4.1 Similarity Evaluation
5.3.4.1.1 Chemical Similarity
5.3.4.1.2 Molecular Similarity
5.3.5 PAINS
5.3.6 Activity Cliffs
5.3.7 Polypharmacology
5.3.8 Drug Repositioning (Drug Repurposing)
5.4 Analog Generation: Pharmaceutical Design
5.4.1 Classical Methods in Pharmaceutical Chemistry
5.4.1.1 Structure-Activity Relationships (SAR)
5.4.1.2 Design of Analogs with Classical Techniques
5.4.1.2.1 Selective Optimization of Side Activities (SOSA)
5.4.1.2.2 Approach with Molecular Fragments (Fragment-Based Discovery)
5.4.1.2.3 Homologous Series
5.4.1.2.4 Stereochemistry in Drugs
5.4.1.2.5 Vinylogy
5.4.1.2.6 Molecular Simplification
5.4.1.2.7 Molecular Complication
5.4.1.2.8 Molecular Doubling
5.4.1.2.9 Isostery
5.4.1.2.10 Scaffold Hopping
5.4.2 Rational Drug Design (Computer Aided Drug Design)
5.4.2.1 Overview (LBDD and SBDD)
5.4.2.2 Ligand-Based Methods (LBDD)
5.4.2.2.1 Pharmacophoric Approach
5.4.2.2.1.1 History, Overview, and Theory
5.4.2.2.1.2 Generation of Pharmacophoric Models
5.4.2.2.1.3 Active Analog Approach
5.4.2.2.1.4 Applications
5.4.2.2.2 Quantitative Structure-Activity Relationships (QSAR)
5.4.2.2.1 History and Early Approaches
5.4.2.2.2 The Hansch/Fujita Method (Quantitative Linear Free Enrgy Relationships)
5.4.2.2.3 The Free-Wilson Method (Quantitative Structure-Activity Relationships)
5.4.2.2.4 Mixed Methods
5.4.2.2.5 Proliferation of Parameters in QSAR
5.4.2.2.6 Evolution and Development of QSAR
5.4.2.2.7 Construction of QSAR Models
5.4.2.2.7.1 Validation of QSAR Models
5.4.2.2.8 3-D QSAR
5.4.2.2.8.1 MIFs in QSAR
5.4.2.2.8.2 Comparative Molecular Field Analysis (CoMFA)
5.4.2.3 Macromolecule Knowledge Based Methods (SBDD)
6 Systematic Pharmaceutical Chemistry
During the study of Structures and Syntheses, the Student should refer to the following directions.
[N] indicates that only the name is to be given
[S] indicates that the synthesis is to be studied.
Also in all cases where the mechanism of action, structure-activity relationships, and pharmacokinetics have been explained the student should consider them as the subject of examination
6.1 Classification of Drugs
6.2 Naming of Drugs
6.3 Antiinfective Drugs
6.3.1 Antibacterial/Antibiotics.
6.3.1.1 History
6.3.1.2 Classification by Mechanism of Action
6.3.1.3 Inhibitors of Metabolite Synthesis
6.3.1.4 Inhibitors of Nucleic Acid Biosynthesis
6.3.1.5 Inhibitors of Bacterial Wall Biosynthesis
6.3.1.6 Inhibitors of Bacterial Protein Biosynthesis
6.3.2 Antifungals
Types of fungi pathogenic to humans, structure and diseases
Classes of drugs used as antifungals and their structures
6.3.2.1 Azole Antifungal Drugs [Structures: Choice of at least one example per generation]
6.3.3 AntiTuberculars
Mycobacterial types pathogenic to humans, structure and diseases
Implications of tuberculosis in the world and history of antituberculars
Selection of MDR and XDR resistant strains
Treatment approaches: first choice, second choice, third choice
Classes of drugs used as antituberculars and their structures[Structures: Choice at least one example per generation-no structures used in multiple chapters allowed]
Antituberculars of the 1940s: Streptomycin, paraamino salicylic acid.
Antituberculars of the 1950s: Isoniazid, Ethionamide, Cycloserine, Prothionamide, Viomycin, Pyrazinamide, Kanamycin.
Antituberculars of the 1960-70s: Thioacetazone, Capreomycin, Clofazimine, Ethambutol, Rifampin.
Antituberculars of the 1980s: Linezolid, Eperezolid.
Antituberculars of the 2000s: Betaquiline[S], Dalamanid[S], Pretomanid, Delpazolid, Sutezolid, Moxifloxacin.
Details on Structure-Activity Relationships of Antituberculars.
Based on the linezolid oxazolidinones
Based on the floroquinolones
Based on betaquiline
Based on clofazimine
Details of the mechanism of action of anti-tubercular drugs.
Mechanisms of Resistance to Antitubercular Drugs.
Toxicity and Pharmacodynamics of Delamanid and other antimycobacterials (Drug Bank)
6.3.4 Antiparasitics.
Classification
Characteristics of the ideal antiparasitic drug
Relevant parasites that cause disease in humans
Protozoa and classification
Helminths and classification
Ectoparasites and classification
Avermectin as a broad-spectrum antiparasite
Antiparasitic therapy
Antimalarial drugs
The genus plasmodium
Mechanisms of resistance
The malaria vector
The physical and chemical forms of prevention
The reproductive cycle of malaria
Points of possible exploitation of the malaria production cycle to generate drugs
Overview of antimalarials and combinations
Antimalarials Quinolinics[Structures: Choice of at least one example per group]
History and derivatives of natural origin: quinine extracts and alkaloids(quinine, quinidine, cinconine, cinconidine)
History and derivatives of synthetic origin: methylene blue and derivatives
Derivatives of the 4-Aminoquinolines: chloroquine[S], Amodiaquine, Isoquine,tert-butylisoquine, piperaquine, ferroquine, pironaridine
Mechanism of action and resensibilisers/hybrids (verapamil, imipramine, dibemetil)
Structure-Activity Relationships
Metabolism and pharmacokinetics (pro-drug metabolites)
8-Aminoquinoline derivatives: pamachin, primaquine[S], tafenoquine, bulachin
Mechanism of action
Structure-Activity Relationships
Metabolism and pharmacokinetics (pro-drug metabolites)
Methanolic derivatives of quinoline: quinine[abbreviated total synthesis], mefloquine, lumefantrine
Mechanism of action.
Structure-Activity Relationships
Metabolism and pharmacokinetics (pro-drug metabolites)
Antimalarials Artemisin derivatives[Structures: Choice of at least one example per group]
History and discovery of artemisinin
Semisynthetic derivatives of artemisinin: artenimol, artemeter, arteeter, artesunate
Mechanism of action
Structure-Activity Relationships
Metabolism and pharmacokinetics
6.3.5 Antivirals
6.3.5.1 General Information.
History and Viruses Pathogenic to Humans
Transfection Animals <--> Humans
Overview of mechanisms of action of antivirals
6.3.5.2 Anti Influenza[Facilities: Choice of at least one example per group]
Generalities
Matrix 2 Inhibitors
Mechanism of Action and Structures
Amantadine, Rimantadine
Polymerase Inhibitors
Mechanism of Action and Structures
Ribavirin, Favipiravir, Balozavir
Neuraminidase inhibitors
Mechanism of Action, Structures and Structure-Activity Relationships
Zanamivir, Laninamivir, Peramivir, Oseltamivir[S]
6.3.5.3 Anti-HIV.
Generalities, virus replicative cycle and drug targets, anti-AIDS therapies (ART and HAART)
Reverse transcriptase inhibitors
Nucleosides (NRTIs)[Structures: Choice of at least one example per group].
Mechanism of action, structure and strength
Zidovudine, Stavudine, Zalcitabine, Didanosine, Emtricitabine, Lamivudine, Abacavir, Tenofovir alafenamide
Non-Nucleosides (NNRTIs)[Structures: Choice of at least one example per group]
Mechanism of action, structure and strength
"Butterfly-like" model: HEPT, TIBO, alpha-APA
"horseshoe-like" model
"Seehorse" model
Nevirapine, Efavirenz, Rilpivirine, Etravirine, Delarvidin, Doravirine[S]
Protease inhibitors[Structures: Choice of at least one example per group]
Mechanism of Action, Structures, and Structure-Activity Relationships
Nelfinavir, saquinavir, Indinavir, Atazanavir, Lopinavir, Tipranavir, Amprenavir, Fosamprenavir, Darunavir[S], Ritonavir, Cobicistat
Integrase inhibitors[Structures: Choice of at least one example per group]
Mechanism of Action, Structures and Structure-Activity Relationships
Raltegravir, Elvitegravir, Dolutegravir, Bictegravir[S], Dolutegravir>
Fusion Inhibitors
Mechanism of Action, Structures
Maraviroc, Enfurfivide[N]
6.3.5.4 Anti-HCV
Generalities, virus replicative cycle and drug targets, anti-HCV therapies (direct acting antivirals - DAAs)
NS5A protein inhibitors[Structures: Choice of at least one example per group].
Mechanism of action, structure and resistance
Ledipasvir, Daclatasvir, Ombitasvir, Elbasvir, Glecaprevir[S], Pibrentasvir
NS5B polymerase inhibitors[Structures: Choice of at least one example per group]
Mechanism of Action, Structures and Structure-Activity Relationships
Beclabuvir, Dasabuvir, Sofosbuvir
NS3/4A protease inhibitors[Structures: Choice of at least one example per group]
Mechanism of Action, Structures and Structure-Activity Relationships
Boceprevir, Telaprevir, Asunanaprevir, Simeprevir, Paritaprevir, Vaniprevir, Grazoprevir, Danoprevir
6.3.5.5 Miscellaneous of Antivirals[Facilities: Choice of at least one example per group]
Generalities, therapies for on HBV, HSV, VZV and HCMV and mechanism of action
5-substituted deoxyuridine analogs: Idoxuridine, Trifluridine, Brivudine
Nucleoside analogs: Telbivudine, Entecavir, Vidarabine, FV100
Pyrophosphate analogs: Foscarnet
Chain terminators
Acyclic nucleosides: Acyclovir[S], Ganciclovir, Penciclovir, Famciclovir, Valacyclovir, Valganciclovir
Phosphonated acyclic nuclesides: Cidofovir, Adefovir, Tenofovir, Tenofovir alafenamide
Fusion inhibitors: Docosanol, palivizumab[N], VariZIG[N], VZIG[N]
6.3.5.6 Anti-COVID19 Drugs.
Generalities about the SARS-CoV-2 virus
Potential Points of Attack in the virus life cycle and molecules studied
Inhibitors of Virus entry: Arbidol, Camostat, Chloroquine, Hydroxychloroquine
Virus replication inhibitors: remdesivir[S], favilavir, ribavirin, lopinavir, ritonavir, nirmatrelvir
Immunomodulatory agents[hint][N].
Drug repurposing as an approach for potential anti-COVID drug discovery19
Principal protease as the main target
The approved drugs for the treatment of COVID19: remdesivir[S], paxlovid, baricitinib, dexamethasone, ritonavir + nirmatrelvir, ritonavir + lopinavir
Drugs proven but not approved for the treatment of COVID19: ivermectin, hydroxychloroquine, azithromycin
The use of drug-drug interactions to potentiate antiviral drugs
6.3.6 Topical and General Antiinfectives
Generalities
Advantages and Disadvantages of using antimicrobials for bacterial skin infections
Types of conditions in which to use topical antifectives
Impetigo
Chronic wounds
Burn wounds
Prevention of post-surgical infections
Prevention of wound infections from minor trauma
Avermectin as a broad-spectrum antiparasite
Antiparasitic therapy
Antiinfectivit Topicals[Structures: Choice of at least two examples per group]
Mupirocin, Fusidic acid, Neomycin, Gentamicin, Aureomycin, Bacitracin, Polymyxin B, Retapamulin
Disinfectants[Structures: Choice of at least one example per group]
Chlorhexidine, Triclosan, Povidone-Iodide, Alcohol, Hydrogen peroxide, Merbromine, Benzalkonium chloride, Chlorhexinol, Sulfadiazine Silver, Mafenide, Silver Proteinate, Silver Coated Fabrics, Aquacel Ag+ (antimicrobial mechanisms of Ag), Chlorchinaldol
Essential Oils]
Activity Types
Indications
Mechanism of Action
6.4 Digestive System Drugs.
6.4.1 Antinausea and Antiemetics
Generalities
Types of pharmacological remedies
6.4.2 Prokinetics and Laxatives
Bulk laxatives:
Osmotic agents: lactulose, methylcellulose, magnesium sulfate
Emollients: Docusate
Nonspecific stimulants[Structures: Choice of at least one example per group]: anthraquinones from cascara sagrada and senna (cascarosides A-D, emodin, barbaloin, sennosides A-D, sennidine A-B)
Prokinetic agents: castor oil, bisacodyl, plecanatide[N], prucalopride
6.4.3 Antidiarrheals
Adsorbents: kaolin-pectin, fiber, charcoal
Alterants of intestinal secretion[Structures: Choice of at least one example per group]: bismuth salicylate, Racecadotril,
Intestinal motility inhibitors[Structures: Choice at least one example per group].
Loperamide, Diphenoxylate
Antispasmodics (Alverine, Mebeverine, Otilonium bromide), Pinaverium bromide
Typical antibiotics[Structures: Choice of at least one example per group]: rifamycin, rifamixin
Hormones: Telotristat, Octretide[N], Somatostatin[N]
Bile acids and facultative resin constructs: cholestyramine[N], colesevelam[N], colestipol[N], Ondasentron[N]
Probiotics: Lactobacillum and Bifidobacterium
Optional 5-HT3-structure antagonists: Alosentron[N], Cliansentron[N], Ramosentron[N], Ondasentron[N]
6.4.4 Antacids and Antiulcer.
Generalities on peptic ulcer (gastric and duodenal)
Implications with Helicobacter Pylori
Anticholinergic agents: Structures and Mechanism of Action (Atropine, Ioscyamine, Scopolamine, Pyrenzepine)
H2 receptor antagonists
History and Development, Mechanism of Action, Structure-Activity Relationships. Pharmacokinetics
Role of H2 Receptors
Structures [Choice of at least one example per group]and Mechanism of Action of Cimetidine, Famotidine, Ranitidine, Nizatidine, Roxatidine, Lafutidine
Specific alpha-2 agonists: clonidine
Proton Pump Inhibitors
History and Development, Mechanism of Action, Structure-Activity Relationships. Pharmacokinetics
Role of HK-ATPase
Structures [Choice at least one example per group] and Mechanism of Action of Omeprazole/Esomeprazole[S], Lansoprazole, Rabeprazole, Pantoprazole
Competitive Potassium Blockers:
Miscellaneous: Structure and Mechanism of Action of Sucralfate, Carbenoxolone, Misoprostol
Carbonic Anhydrase Inhibitors: Acetazolamide
6.4.5 Therapy of Irritable Bowel Syndrome
6.4.6 Therapy of Chronic Intestinal Inflammation.
5-Amino-salicylic acid derivatives: 5-ASA, Balsalazide, Olsalazine, Sulfasalazine
Immunosuppressive agents: Azathioprine, Mercaptopurine, Methotrexate
Tumor Necrosis Factor antagonists: AdalimumabN, CertolizumabN, GolimumabN, InfliximabN
Miscellaneous: Metronidazole and NatalizumabN
6.4.1 Antinausea and Antiemetics
6.5 Antitumor Drugs
6.5.0 Generalities on antitumor therapy.
6.5.1 Classical Antitumor Drugs
Alkylating Agents
Azotate mustards [chlormetine, cyclophosphamide, chlorambucil]
Ethylenamines and methylenamines [altretamine]
Alkyl sulfonates [busulfan]
Nitrosoureas [carmustine, lomustine]
Platinum derivatives [cisplatin]
Cytotoxic antibiotics [Bleomycin, Anthracyclines {Doxorubicin, epirubicin, idarubicin and valrubicin}, Mitomycin]
Antimetabolites
Antifolates [Methotrexate, Pemetrexed, Pralatrexate, Trimetrexate]
Purine analogs [Azathioprine (Mercaptopurine, Thioguanine)]
Pyrimidine analogs [Azacitidine, Decitabine, ]
Taxanes [Paclitaxel[S], Cabazitaxel, Docetaxel]
Topoisomerase inhibitors
Topoisomerase I [Irinotecan, Topotecan, Camptothecin]
Topoisomerase II [Etoposide, teniposide, podophyllotoxin]
Vinca alkaloids [vincristine, vinblastine, vinorelbine]
6.5.1 Modern Antitumor Agents
HDAC inhibitors [Belinostat, Panobinostat, Romidepsin, Vorinostat[S], Tucidinostat]
Antiandrogens [cyproterone acetate, Abiraterone acetate, flutamide, nilutamide, bicalutamide]
Aromatase inhibitors [anastrozole, letrozole, exemestane]
Kinase inhibitors [Imatinib, Sorafenib, Dabrafenib]

Adopted texts

The studying material for the course:
- Foye's. Principi di chimica farmaceutica 2021 Edition
- Chimica Farmaceutica di Patrick L. Graham 2015 Edition
- Materiale didattico comprensivo di:
-- Copy of the power point presentation in pdf format
-- Scientific Publications

Bibliography

See above

Prerequisites

The students should have acquired the content of all courses followed in the previous years with particular indication to all chemisty based and biochemistry courses. Medicinal chemistry rely on fundamental courses and therefore it is very important their knowledge In particular to easily follow the lectures the sudent should have acquired the following exams: Mathematics Physics Physical Chemistry Analitical Chemistry Organic Chemistry I Organic Chemistry II Biochemistry Pharmacology (for this is requested to the students to follow the lectures running in parallel)

Study modes

Theoretical face-to-face lectures during which slides are projected that the student has available as teaching material via link to elearning.uniroma1.it. The slides serve as the basis for detailed explanations by the lecturer on the various topics of the course, in particular, the synthesis and mode of action of the drugs examined are addressed in depth. Thus, with lecture attendance and available files, the student has the necessary course material for exam preparation. Both face-to-face lectures and examinations may be conducted remotely in telematic mode. In addition, the lecturer provides several scientific publications for the details addressed during the lectures

Frequency modes

Lectures are in the classroom where the teacher encourages students to actively participate

Exam modes

For the final exam the student will face a written test with open questions focused on sistematic medicinal chemistry: chemical structures, structure-activity relationship, chemical synthesis and pharmacokinetcs of drugs seen during the course and listed in the program. The written test will enable to the oral part in which the student will be interrogated on the general medicinal chemistry part (drug discovery and design)

Exam reservation date start	Exam reservation date end	Exam date
10/01/2024	20/01/2024	02/02/2024
03/02/2024	18/02/2024	26/02/2024
26/02/2024	20/04/2024	29/04/2024
30/04/2024	01/06/2024	10/06/2024
11/06/2024	23/06/2024	01/07/2024
02/07/2024	25/08/2024	03/09/2024
04/09/2024	20/09/2024	30/09/2024
01/10/2024	24/10/2024	04/11/2024
05/11/2024	03/12/2024	13/12/2024
14/12/2024	01/01/2025	09/01/2025