Teaching - Università degli Studi della Tuscia

Chimica delle sostanze bioattive (objectives)

EXPECTED LEARNING RESULTS

• Knowledge and understanding: Knowledge of the principles that define the minimum structural unit of an organic, natural or synthetic molecule, to have a certain biological activity (pharmacophore theory). Knowledge of the relationship between the type of pharmacophore present in an organic molecule and the pharmaceutical and pharmacological activity. Knowledge ot the molecular-level of the action mechanism of the major families of bioactive substances, with particular attention to substances with antioxidant, antiviral, anti-inflammatory and antitumour activity. Knowledge of the key steps for the design of a drug, and procedures for its clinical validation and use. Knowledge of the origin and distribution in nature of the main families of biologically active natural organic substances.
• Applied knowledge and understanding: In addition to the knowledge gained through the bioactive substance chemistry study, students will be able to apply theoretical concepts acquired during the course in solving practical exercises based on the teacher's request to present possible schemes for the design of a drug, having the initial indication of the target of action at the molecular level and knowing the type of pathology against which the treatment therapy is to be developed. In this case, students will also have to apply their previous knowledge of chemistry and biology for complete resolution of the problem.
• Making judgements: At the end of the course, the student will have acquired the necessary training for full autonomy of judgment on the possibility of using a certain organic substance of natural or synthetic origin for the therapy of a certain pathology . The student will then be able to link the acquired knowledge of biochemistry, molecular biology, enzymology, physiology and genetic to the design of a substance applicable in the pharmaceutical, nutraceutical and cosmeceutical fields.
• Communication skills: students will be continuously and consistently invited to participate actively in the lesson in order to deepen the topic and to collect proposals for possible solutions in the case of complex phatological scenarios. In this activity, students will be called upon to meet in order to support their ideas. The educational pitch is aimed at increasing the communicative skills and the ability to know how to work and to confront a group, all aimed at consolidating the acquired concepts.
• Learning Skills: Students' learning abilities will be evaluated during the course of the course by tests that will allow to individually monitor the maturation state of the knowledge, highlighting the student's ability to return the aquired cencepts.

Code

18436

Language

ITA

Type of certificate

Profit certificate

Credits

Scientific Disciplinary Sector Code

CHIM/06

Contact Hours

Type of Activity

Core compulsory activities

Teacher	BOTTA Lorenzo (syllabus) General Section Definition of drug. Pharmacokinetics: absorption, distribution, metabolism and elimination. Physico-chemical properties of the drug that influence each of these phases. Bioavailability and bioequivalence concepts. Cell membrane properties. Fatty acids: classification, properties and biological role. Pharmacodynamics. Receptor: definition and characteristics. Classification of receptors. Receptor site and its specificity. Allosteric and accessory sites. Ligand-receptor interaction: role of the chemical bond in the receptor interaction. Ionotropic receptors: structure and characteristics. Drug targets: Proteins, Enzymes, Receptors and Nucleic Acids: structure and function. Receptors and signal transduction. Receptor activation mechanisms: ionotropic; voltage-dependent and ligand-dependent; receptor activated by phosphorylation. G protein coupled receptors: structure and activation of the G protein cycle. Role of the α portion of the G protein. Effectors of the α portion and effects mediated by Gs, Gi, Gq. Structure and functional groups of the main endogenous ligands of ionotropic and metabotropics receptors: Gaba, Glycine, Aspartate, Glutamate, Acetylcholine, Adrenaline, Noradrenaline, Serotonin, Dopamine, Histamine. Protein kinase receptor. Transmembrane single strand GTPase receptor. The pharmacophore and the molecular outline of a drug. Concept of affinity and intrinsic activity. Definition of agonist, partial agonist, inverse agonist, antagonist. Cellular excitability. Mechanism of propagation of the impulse. Chemical synapses: structure, role of vesicles, mechanisms of synthesis and storage of the mediator, release of the mediator. The postsynaptic receptors. Mechanism of presynaptic reuptake of the mediator. Characteristics of the receptor site of the main neurotransmitters: Serotonin, Dopamine, Histamine, Acetylcholine, Noradrenaline. Drug-receptor interactions. Electronic interactions. Bonds involved in the drug-receptor complex: covalent bond, ionic bond, hydrogen bond, charge transfer complexes, Van der Waals forces and other interactions. Steric interactions: steric effects in the drug-receptor complex. Computational Chemistry: Molecular Modelling (conformational analysis, identification of the 3D pharmacophore), Docking, Virtual Screening, Homology Modelling, Pseudoreceptors, De novo drug design. Formulation and delivery of drugs: principles and use of specific carriers (liposomes, micelles, antibodies, lignin). Special Part Antiviral agents: nucleic acids structure and properties, drugs against DNA and RNA viruses, antisense oligonucleotides, broad spectrum drugs, vaccines Antitumor agents: drugs that act on nucleic acids (intercalants, topoisomerase poisons, alkylating and metalizing agents, chain terminator), antisense therapy, drugs that act on enzymes (adrenergic antagonists, antimetabolites), antibodies and antibody-drug conjugates. (reference books) Chimica farmaceutica di Patrick L. Graham Chimica farmaceutica di Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre
Dates of beginning and end of teaching activities	From 01/03/2021 to 11/06/2021
Delivery mode	Traditional At a distance
Attendance	not mandatory
Evaluation methods	Oral exam