Ateneo - UPO

The course focuses on the in-depth study of different classes of drugs, considering the rationale behind their discovery, mechanisms of action, structure–activity relationships, and therapeutic applications. In particular, the following classes of drugs will be examined: cholinergic agents, adrenergic agents, anti-Parkinson drugs, antipsychotics, antidepressants, anxiolytics, sedative-hypnotics, antihypertensives, antihistamines, anticoagulants, oral hypoglycemic agents, analgesics (NSAIDs and opioids), steroid hormones and related drugs, anticancer agents, antibacterial agents, and antiviral agents.

A. Gasco, F. Gualtieri, C. Melchiorre Chimica Farmaceutica (I Eds.) Casa Editrice Ambrosiana; W. Foye, Principi di Chimica Farmaceutica, Piccin; (VI Eds.); Wilson and Gisvold, Chimica Farmaceutica (I Eds.) Casa Editrice Ambrosiana; G.L. Patrick Introduzione alla Chimica Farmaceutica (edizione integrata) EdiSES. T.L. Lemke, D.A. Williams. Foye’s, Principi di Chimica Farmaceutica, V Eds. Piccin; G. Costantino, G. Sbardella, EDISES;

The goals of the course of Medicinal Chemistry and Drug Design II are:
- To provide students with the fundamental knowledge of the drug classes discussed and at the same time the general strategies for their design, the study of their mechanisms of action at the molecular level, their chemical- toxicological aspects and their relationships between chemical structure and biological activity. At the end of the course, the student will have gain a deep knowledge concerning these classes of drugs, in particular with regard to their mechanism of action at the chemical level. At the end of the course, the student will be able to read, in a critical manner, books and scientific articles regarding these classes of drugs.

Regarding preparatory Pharmaceutical Chemistry and Drug design I
Preliminary matters Knowledge in the field of Organic Chemistry, General Pathology, Biochemistry, Physiology, Pharmacology.

Frontal Seminar

Students with physical disabilities, Learning Disabilities or Special Education Needs can request specific services and tools via the Staff Sviluppo e Coordinamento Carriere e Servizi alle Studentesse e agli Studenti, consulting the University webpage: https://www.uniupo.it/en/services/services-students-physical-or-learning-disabilities Students with disabilities, learning disabilities or special education needs, once they have contacted the University Staff, can refer to the tutor in charge of the course to define the examination modalities, concerning academic aspects.

The learning assessment consists of a written examination. The questions cover all the topics which have been discussed during the lessons.

The course covers the study of antibacterial agents, including bacterial cell structure, differences between Gram-positive and Gram-negative bacteria, the bacterial cell wall, and mechanisms of antimicrobial resistance. The following classes of antibacterial drugs are examined: sulfonamides, sulfones, dihydrofolate reductase inhibitors, penicillins, cephalosporins, carbapenems, monobactams, β-lactamase inhibitors, glycopeptides, fosfomycin, polymyxins, daptomycin, aminoglycosides, tetracyclines, chloramphenicol, macrolides, lincosamides, oxazolidinones, quinolones and fluoroquinolones, as well as the major antitubercular agents.Antiprotozoal drugs used in the treatment of amoebiasis, giardiasis, trichomoniasis, leishmaniasis, and trypanosomiasis are discussed, with particular emphasis on metronidazole, nitazoxanide, paromomycin, antimonial compounds, eflornithine, nifurtimox, and benznidazole. Antimalarial drugs are also covered, including cinchona alkaloids, 4-aminoquinolines, 8-aminoquinolines, 9-aminoacridines, artemisinin derivatives, synthetic ozonides, antifolates, and atovaquone.The course also includes antifungal drugs, with a focus on echinocandins, amphotericin B, azoles and triazoles, squalene epoxidase inhibitors, griseofulvin, and inhibitors of nucleic acid synthesis, as well as anthelmintic agents such as praziquantel, niclosamide, albendazole, ivermectin, and related compounds. General principles of antiviral chemotherapy and the major pharmacological targets involved in the viral replication cycle are also introduced.With regard to drugs affecting glucose metabolism, the course addresses insulin and glucagon physiology, diabetes mellitus and its complications, modified insulin preparations, sulfonylureas, meglitinides, biguanides, α-glucosidase inhibitors, thiazolidinediones, DPP-IV inhibitors, and GLP-1 receptor agonists.Within the field of drugs acting on hemostasis, platelet aggregation and blood coagulation mechanisms are examined, together with antiplatelet agents, heparins, fondaparinux, direct thrombin inhibitors, factor Xa inhibitors, vitamin K antagonists, thrombolytic agents, and antihemorrhagic drugs.A substantial portion of the course is devoted to steroid hormones and their chemistry. Topics include steroid structure, stereochemistry and nomenclature, biosynthesis of steroid hormones, natural and synthetic estrogens, nonsteroidal estrogens, selective estrogen receptor modulators, antiestrogens, aromatase inhibitors, progestins, oral contraceptives, androgens, anabolic steroids, antiandrogens, 5α-reductase inhibitors, glucocorticoids, mineralocorticoids, and aldosterone antagonists.Analgesic and anti-inflammatory drugs are studied with particular emphasis on the pathophysiology of inflammation, the arachidonic acid cascade, prostaglandins, and thromboxanes. The major classes of nonsteroidal anti-inflammatory drugs (NSAIDs) are examined, including salicylates, anthranilic acid derivatives, anilines, pyrazolones, oxicams, arylacetic acid derivatives, arylpropionic acid derivatives, and selective COX-2 inhibitors.Within the area of central nervous system drugs, the course addresses the pathophysiology of epilepsy and the major classes of anticonvulsants, including hydantoins, iminostilbenes, succinimides, oxazolidinediones, valproic acid, benzodiazepines, barbiturates, tiagabine, vigabatrin, gabapentin, pregabalin, and felbamate. Antipsychotic drugs are also studied, with particular attention to the dopaminergic and serotonergic theories of schizophrenia, typical and atypical neuroleptics, and their structure–activity relationships.Cholinergic and anticholinergic drugs are examined, including the biosynthesis, release and metabolism of acetylcholine, muscarinic and nicotinic receptors, cholinergic agonists and antagonists, acetylcholinesterase inhibitors, and their principal therapeutic applications. Drugs used in the treatment of Alzheimer’s disease are also discussed, including tacrine, donepezil, rivastigmine, galantamine, and modulators of the glutamatergic system.For adrenergic drugs, the course covers the biosynthesis and metabolism of epinephrine and norepinephrine, classification and distribution of α- and β-adrenergic receptors, adrenergic agonists and antagonists, the structure–activity relationships of catecholamines and their analogues, α1-, α2-, β1-, β2-, and β3-agonists, and their therapeutic applications.Within the field of antidepressant drugs, the neurochemical basis of depression is examined together with tricyclic antidepressants, monoamine oxidase inhibitors, selective serotonin reuptake inhibitors, and mood stabilizers.For antiparkinsonian drugs, the course addresses the pathophysiology of Parkinson’s disease, therapeutic strategies aimed at enhancing dopaminergic neurotransmission, levodopa, DOPA-decarboxylase inhibitors, dopamine agonists, MAO-B inhibitors, COMT inhibitors, and muscarinic antagonists.The course also covers anxiolytic and sedative-hypnotic drugs, with particular emphasis on benzodiazepines, serotonin and buspirone, sleep physiology, melatonin and its analogues, barbiturates, piperidinediones, succinimides, quinazolinones, and the structure–activity relationships of hypnotic agents.General anesthetics are examined, including theories of anesthesia, inhalational anesthetics, intravenous anesthetics, and preanesthetic medications. Local anesthetics are also discussed, with emphasis on sodium channel blockade, cocaine, ester- and amide-type local anesthetics, lidocaine and its analogues, and the structure–activity relationships of local anesthetic agents.Finally, opioid analgesics are studied, including pain physiology, the nociceptive system, opioid receptors, opium alkaloids, morphine, codeine, thebaine, semisynthetic and synthetic derivatives, opioid agonists, partial agonists, and antagonists, with particular emphasis on structure–activity relationships.The course is completed by cardiovascular drugs, including osmotic diuretics, carbonic anhydrase inhibitors, loop diuretics, thiazide diuretics, potassium-sparing diuretics, antihypertensive drugs, inhibitors of the renin–angiotensin–aldosterone system, ACE inhibitors, angiotensin II receptor antagonists, calcium channel blockers, and the principal cardiotonic and lipid-lowering agents.

The students at the end of the course will know fundamental aspects regarding specific drug classes. In particular, the student will be able to recognize the general strategies for their design, the study of their mechanisms of action at the molecular level, their chemical- toxicological aspects and their relationships between chemical structure and biological activity. As ultimate goal the student will be able to read, in a critical manner, scientific articles regarding these classes of drugs.