Principles of medicinal chemistry. Physico-chemical properties and biological activity. Principles of pharmacokinetic. Structure-activity relationships. Drug discovery. Principles of pharmacodynamic. Introduction to chemotherapy. Synthetic antibacterial agents. Beta-lactam antibiotics. Antiviral agents. Anti tumor agents. Basic principles of central and peripheral nervous drugs. Cholinergic and anticholinergic agents. Adrenergic and antiadrenergic agents.
1) Chimica Farmaceutica, a cura di A. Gasco, F. Gualtieri,C. Melchiorre. Casa editrice Ambrosiana.
2) Foye's Principi di Chimica Farmaceutica, VII Italian edition, Piccin Nuova Libraria S.p.A., Padova, 2021.
3) Wilson & Gisvold: Chimica Farmaceutica, I edizione italiana, CEA Casa Editrice Ambrosiana, Rozzano, Milano
4) Patrick G. L.: Introduzione alla Chimica Farmaceutica, EdiSES, Napoli, 2010.
Learning Objectives
The course is aimed to teach the principles of Medicinal Chemistry necessary for understanding the design of drugs and the molecular mechanisms for their biological activity. The teaching is organized in theoretical lessons and the programme is divided into a general part which describes the methodologies underlying the discovery of drugs, the relationships between the chemical-physical properties and the structure of the molecules with the pharmacological properties and the phenomena of absorption, distribution, metabolism, excretion and toxicity (ADMET) (3 CFU), and a part in which some classes of drugs taken as representative are described (3 credits)
The knowledge acquired in the course allows the student to understand the influence of the chemical-physical and structural properties of drugs on their pharmacokinetic and pharmacodynamic behaviour which influences their biological behaviour.
Prerequisites
To take the exam it is required to take Physiology and Organic Chemistry exams
Teaching Methods
Lessons in a classroom, using PowerPoint presentations
Further information
e-mail: elisabetta.teodori@unifi.it
Dipartimento di NEUROFARBA, Sezione di Farmaceutica e Nutraceutica, Via U. Schiff 6 50019 Sesto F.no, Firenze, Tel. 055 4573693.
Type of Assessment
There are at least 6 official exam sessions, 3 in the winter session (January-February), 3 in the summer session (June-September); there are also 2 exam sessions in the teaching silence periods in the two semesters. The final exam consists of a written test and an in-depth oral exam. The questions are aimed at ascertaining the level of knowledge and skills acquired concerning the fundamental aspects of medicinal chemistry, the ability to apply its general concepts and to analyze its structure-activity relationships to obtain information on the mechanism of interaction with the biological target. The final evaluation will also take into account the property of the language, the clarity of the exposition and the ability to connect the various topics.
In assigning the final mark, expressed out of thirty, reference will be made to the evaluation grid available on the CdS website (Didactics-Criteria for attributing the exam mark).
The dates of the exam sessions can be consulted on the web page prepared for online enrolment.
Course program
General part (3 CFU): Introduction to Medicinal Chemistry: drugs classification, drug action phases. Physical-chemical properties: ionization, partition coefficient, electron distribution, Interactions involved in drug action: Ionic bond, Van der Waals bond, dipolar bond, hydrogen bond, charge transfer bond, hydrophobic bond, covalent bond, pi-cation bond, chelation bond. Pharmacokinetics: absorption, distribution, metabolism, excretion. Structural characteristics and biological activity: geometric, optical, conformational isomerism. Pharmacodynamics: nucleic acids, enzymes, ion channels, receptors (agonists, antagonists, ligand-receptor interaction models). Drug research and development: drug discovery, rational design, combinatorial chemistry, optimization for molecular manipulation (structure-activity relationships. isosteric substitutions, molecular simplification, molecular complication, physico-chemical modulation, derivatization (prodrugs).
Special part (3 CFU): Introduction to Chemotherapy: mechanism of action of chemotherapy, drug resistance, superinfections. Synthetic antibacterials: sulfonamides, quinolones, DHF reductase inhibitors. Antibiotics: beta-lactam antibiotics. Antivirals: active antiviral chemotherapy: on extracellular viruses; on the penetration phase, on the replication phase (antimetabolites), on the encapsulation phase, on the induction of interferon. Anticancers: alkylators, antimetabolites, DNA intercalators, antibiotics, steroid hormones and antihormones, specific protein complexing agents, targeted anticancer agents. Introduction to central and peripheral nervous system drugs: axon conduction, synaptic conduction, neurotransmitters, central and peripheral nervous system. Cholinergics: acetylcholine biosynthesis, cholinergic synapse, muscarinic and nicotinic receptors, muscarinic agonists, nicotinic agonists, acetylcholinesterase inhibitors. Anticholinergics: muscarinic antagonists, nicotinic antagonists. Adrenergics: adrenaline and noradrenaline biosynthesis, metabolism, adrenergic synapses, alpha and beta receptors, alpha-adrenergic agonists, beta-adrenergics, indirect adrenergic drugs. Antiadrenergics: alpha-antagonists, beta-antagonists, indirect antiadrenergic drugs.