CHIMICA FARMACEUTICA E DEI PRODOTTI NATURALI
Academic Year 2025/2026 - Teacher: LOREDANA SALERNOExpected Learning Outcomes
The course aims to provide students with the tools to study the fundamental concepts that characterize Pharmaceutical Chemistry
Applying knowledge and understanding
The student acquires knowledge of the strategies used for the discovery and design of new active ingredients, of the steps necessary for the development of these drugs and for their development as medicaments. In addition, he will have knowledge of the moments of the action of the drugs and of the natural products, from administration to elimination and of the conditioning properties of the drug-two-phase interaction. The student will have knowledge of selected classes of drugs and natural products and will understand how they interact with neurotransmitter receptors, with intracellular receptors, with enzymes and with ion channels, deepening their mechanisms of action, chemical-pharmaceutical and toxicological properties, and structure-activity relationships
EXPECTED LEARNING RESULTS
The student will know and understand the issues related to the design, the mechanism of action at the molecular level, drug-receptor or natural substaces-receptor interactions, toxicity, metabolism and structure-activity relationships of the classes of drugs examined, in particular those of origin natural
Course Structure
Required Prerequisites
Attendance of Lessons
The course consists of 42 hours of lectures (6 credits) and 12 hours of classroom exercises (1 credit).
Attendance, as per the teaching regulations, is mandatory for at least 70% of the course lessons, assessed in all their forms.
If the course is taught in a blended or distance learning format, any necessary changes to the previously stated curriculum may be made in order to comply with the planned program and the syllabus.
Detailed Course Content
Definition and objectives of Pharmaceutical Chemistry, history and evolution. Discovery of drugs from natural products. Definition of drug. Different ways to classify drugs. ATC classification of drugs. Nomenclature of drugs. Stages of drug and natural products action: pharmaceutical, pharmacokinetics, pharmacodynamics. Pharmacokinetics: absorption, metabolism (phase I and phase II), distribution and elimination of a drug/natural products. Pharmacodynamics: Drug (natural products) targets. Molecular drug (natural products) -target interaction: description of the different chemical bonds involved in the interaction. Receptors: G protein coupled receptors, receptors with intrinsic enzymatic activity, ion channels ligand-gated and voltage-gated. Enzymes and enzymatic inhibition, competitive and non-competitive inhibitors. Nucleic acids. Lipids. Carbohydrates. Discovery, design and development of drugs. Optimization of interaction with the target. Optimization of target access. Prodrugs and Softdrugs. The introduction of drugs on the market.
SYSTEMATIC PART
Examples of drugs derived from natural substances (the following examples will be integrated in class).
OPIOID ANALGESICS. Introduction. Morphine: structure and properties, structure-activity relationships. Opioid receptors, development of morphine analogues, agonists, antagonists.
ANTICANCER. General information on neoplastic diseases and therapeutic approaches, classification of anticancer drugs. Plant-based anticancer drugs
Textbook Information
1. G.L. PATRICK, Chimica Farmaceutica, III Edizione italiana, EdiSES, Napoli, 2015
2. T.L. LEMKE et al., Foye's L'essenziale, Principi di Chimica Farmaceutica, I Edizione italiana, Piccin,
Padova, 2017.
3. R.B. Silverman, M.W. Holladay., Manuale di chimica farmaceutica, progettazione, meccanismo d'azione e metabolismo dei farmaci. Edra
4. G.Costantino, G. Sbardella, Chimica Farmaceutica, Edises Università, 2024
5. Slides of the lessons
Course Planning
| Subjects | Text References | |
|---|---|---|
| 1 | all the topics | reference texts and slides provided by the teacher |
Learning Assessment
Learning Assessment Procedures
The assessment consists of a written exam comprising multiple-choice and open-ended questions.
The exam is designed to assess the student's knowledge of the basic concepts of medicinal chemistry, as well as the fundamental aspects of design, molecular mechanisms of action, and structure-activity relationships (SARs) of the drug classes and natural substances covered during the course.
Classroom exercises will be offered throughout the course, following the same format as the exam.
The assessment may also be conducted online, if circumstances warrant.
Information for students with disabilities and/or learning disabilities (LD): To ensure equal opportunities and in compliance with applicable laws, interested students may request a personal interview to plan any compensatory and/or dispensatory measures, based on their learning objectives and specific needs. You can also contact the CInAP (Center for Active and Participatory Integration - Services for Disabilities and/or DSFS, prof.ssa santina Chiechio
Examples of frequently asked questions and / or exercises
- polar
- nonpolar
- ionic
- buffered
- dissociated
- irreversibly blocking an allosteric site
- binding to the receptor without activating it
- producing a response without binding to a receptor irreversibly
- blocking a receptor binding to the receptor by activating it
- oxidation-reduction, hydrolysis
- conjugation with glucuronic acid
- phosphorylations
- conjugation with the tripeptide glutathione
- alkylation